Ohio State Navbar

People

Karl Werbovetz, PhD


Staff photo

500 W 12th Ave
Columbus, OH 43210

Phone: (614) 292-5499

Email: werbovetz.1@osu.edu

 

Current OSU Appointment

Professor, Pharm CBO/Coll

 

Advising Narrative

Jason Young was in my lab from 2010 to 2012. Jason earned a BS in Neuroscience and also prepared nine new compounds based on a hit negative allosteric antagonist of the nicotinic acetylcholine receptor. He presented a poster entitled Synthesis of Allosteric Modulators for Nicotinic Acetylcholine Receptors at both the Denman Undergraduate Research Forum and at the College of Pharmacy Research Day in May 2012, and also successfully completed an undergraduate Honors thesis at the end of spring 2012. We plan to publish Jason’s work, either as part of a larger body of research or as a brief communication. Jason began medical school at the University of Toledo in August 2012.

Shawn Rito evaluated various compounds for activity against Leishmania parasites from 2009 to 2010. During that time, Shawn measured the efficacy of flavonoids isolated from Mimulus bigelovii by Manar Salem. For his contribution to this project, Shawn was listed as an author on Manar’s recent paper (Phytother. Res. (2011) 25: 1246). Shawn is currently a PharmD student in our College.

Matthew Welsch was an undergraduate researcher in my lab from 2008 to 2009. Matt synthesized six compounds based on a hit from a Leishmania tubulin screen carried out in my lab, but unfortunately these compounds were inactive against this parasite protein. He then made a valiant attempt to prepare 7-substituted-8-methoxyquinolines as candidates against a Leishmania target protein (UDP-glucose pyrophosphorylase). Matt is currently a graduate student in the Chemistry Department at Columbia University.

Joshua Manley conducted undergraduate research in my lab in 2007. He prepared and characterized two nitrile-containing dihydroquinoline target compounds under the direction of postdoc Jean Fotie and attempted to make amidine-containing compounds from these nitriles. Based on his contribution, he was listed as an author on Jean’s dihydroquinoline paper that was published in the Journal of Medicinal Chemistry (J. Med. Chem. (2010) 53: 966).

Sandra Nzimiro performed research in my lab as both a graduate student and as a PharmD student from 2005 to 2007 and successfully defended an undergraduate Honors thesis in 2006. She is also an author on a paper from our lab (Bioorg. Med. Chem. Lett. (2008) 18: 247) in which she demonstrated the dramatic effect of the antiprotozoal diamidine compound DB1111 on the mitochondrion in Leishmania donovani using electron microscopy. Sandra obtained her PharmD and MPH degrees in 2011 from OSU.

Postdoctoral / Researcher Advising

Xiaohua Zhu is currently a senior researcher in my lab. She was hired as a postdoctoral biologist in 2007 and was promoted in 2011. Since she began work in my lab, Xiaohua's skills with in vitro and in vivo antiparasitic assays have served as the core of the antileishmanial compound evaluation efforts for the Consortium for Parasitic Drug Development. Xiaohua is listed as an author on ten papers from our lab (two first author), and more are on the way.

Carolyn Reid was a postdoctoral chemist in my lab from 2008 to 2010. She was involved in synthesizing both dihydroquinoline and arylimidamide antiparasitic compounds, and she has published first author papers on both of these topics. Carolyn is currently a postdoc in the Chemistry and Biochemistry Department at the Ohio State University and is beginning to look for academic positions.

Molla Endeshaw was a postdoctoral chemist in my lab from 2007 to 2008 before obtaining a full-time position at Chemical Abstracts (a position that he still holds). He couldn't stay away from the lab, however, and has worked part-time in my lab since 2010. Molla is an excellent synthetic chemist who has published two papers from my lab (one first author), and at the time of writing this dossier, he has a first author manuscript that is close to submission.

Jean Fotie joined my lab in 2006 as fellow supported by a two year World Health Organization grant. He synthesized a series of trypanocidal dihydroquinoline compounds which were reported in comprehensive first author paper appearing in the Journal of Medicinal Chemistry (J. Med. Chem. (2010) 53: 966) and was also an author on three other papers from our lab. Jean is currently an assistant professor in the Department of Chemistry and Physics at Southeastern Louisiana University.

Rachel Morgan was a postdoctoral research associate in my lab from 2006 to 2008. She worked at the chemistry-biology interface, performing a screen of 10,000 compounds against Leishmania tubulin and also conducting synthetic chemistry in the lab. Rachel was the first author of a review paper from my lab and was also the first author of a paper describing her tubulin screen in addition to being an author on three other papers from our lab. She is currently a postdoc at King's College London.

Tesmol George was a postdoctoral chemist in my lab from 2004 to 2006. She was also very proficient in making and characterizing new target compounds, mainly to support our investigation of tubulin as an antiparasitic drug target. Tesmol published four papers while in my lab, three of which were first author contributions. Tesmol is now employed as a senior scientist at PKC Pharmaceuticals, Woburn, MA.

Gautam Bhattacharya was a postdoctoral research associate in my lab from 2001 to 2003. He was an excellent medicinal chemist who published three first author papers and five papers in total while in my lab. The majority of his time was spent on the synthesis of antiparasitic antimitotic agents, and I believe that his first author paper in the Journal of Medicinal Chemistry (J. Med. Chem. (2004) 47:1823) was instrumental in our lab obtaining an R01 grant on this topic. To the best of my knowledge, Gautam's most recent position was as a research scientist at Chembiotek Research International in Calcutta.

Master/Graduate Advising

The graduate and undergraduate students who have worked in my lab are listed in sections 2a) and 2b). Below please find the Ohio State students for whom I have served on their graduate committees.

Doctoral Students (dissertation committee member summer 2006-present): 10

Su-Lin Lee, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Ching-Shih Chen, 2012)
Kiran Mahasenan, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Chenglong Li, 2012)
Dalia Abdelhamid, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. James Fuchs, 2011)
Mark Bahar, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. A. Douglas Kinghorn, 2012)
Rohit Tiwari, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Werner Tjarks, 2010)
Yu-Yu Liu, Ohio State Biochemistry Program, The Ohio State University (advisor - Dr. Sissy Jiang, 2010)
Anuradha Kalyanasundarum, Integrated Biomedical Science Graduate Program, The Ohio State University (advisor - Dr. Muthu Periasamy, 2009)
Weihong Qiu, Department of Physics, The Ohio State University (advisor - Dr. Dongping Zhong, 2008)
Wendy Rich, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Robert Brueggemeier, 2008)
Bulbul Pandit, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Tom Li, 2007)

Masters Students (committee member 2007-present): 1

Heng Chiat Tai, Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University (advisor - Dr. Chenglong Li, 2009)

Doctoral Students (general examination committee member Summer 2006 - present): 17

Wenying Yu, 2012
Charlie Pyle, 2012
Yong Chen (Department of Chemistry and Biochemistry), 2011
Tien-Lu Huang, 2011
Lynette Bueno-Perez, 2011
Jie Li, 2011
Bitna Yi, 2011
Jonathan Etter, 2010
Deepak Bhasin, 2010
Kiran Mahasenan, 2010
Dalia Abdelhamid, 2009
Su-Lin Lee, 2009
Sunjoo Ahn, 2008
Nicholas Regan, 2008
Rohit Tiwari, 2007
Mark Bahar, 2007
Joshua Fletcher, 2007

Academic Advising

Graduate students, postdocs, and undergraduate students conducting research in my laboratory discuss their progress with me on a regular basis and present their work at lab meetings. Undergraduate BSPS students that have nominally been listed as my advisees rarely seek my guidance. However, on such occasions, I attempt to give these students a "big picture" view of their career choices.

Noteworthy Graduate Narrative

Eight graduate students have been under my supervision: Manar Salem (Ph.D., 2005), Dawn Delfin (Ph.D., 2007), Adam Yakovich (Ph.D., 2007), Mitali Mukherjee (left without a degree, 2007), Kirk Latibeaudiere (M.S., 2008), Shanshan He (Ph.D., 2012), Trupti Pandharkar (sixth year), and Julian Richard (fifth year).

Trupti Pandharkar began her graduate career in the Division of Medicinal Chemistry and Pharmacognosy in spring 2007. During that time, she has served as a teaching assistant, as an administrative assistant helping to assemble the College of Pharmacy Technology Portfolio, and as an integral part of our antileishmanial compound evaluation efforts with the Consortium for Parasitic Drug Development. Her efforts in antileishmanial compound evaluation have resulted in her inclusion as an author on four papers from our lab. Trupti is currently working on a first author manuscript and is on schedule to graduate by the end of 2012.

Shanshan He enrolled in the Medicinal Chemistry and Pharmacognosy graduate program in fall 2007. She was awarded the Jane Chen graduate fellowship, served as a teaching assistant, and also helped to assemble a portfolio containing the intellectual property of our OSU College of Pharmacy as an administrative assistant during her graduate career. Her first author paper describing the most important findings of her dissertation research was published in Antimicrobial Agents and Chemotherapy earlier this year, and a poster describing this work won a student poster award at the 2012 Keystone Drugs against Parasitic Protozoans meeting. She is also an author on two other papers from our lab. Shanshan spent the summer of 2011 as an intern at Pfizer in Kalamazoo, MI. She defended her dissertation in June 2012 and is currently working on hepatitis C virus as a postdoc in Dr. Jake Liang's lab at the National Institutes of Health.

Adam Yakovich began his graduate career in the Division of Medicinal Chemistry and Pharmacognosy in fall 2002. He was an author on six papers from our lab during his time as a graduate student, including one first author paper. After completing his dissertation in 2007, he accepted a postdoctoral position in Dr. John Barnard's lab in the Center for Cell and Developmental Biology at Nationwide Children’s Hospital. Adam has published three papers as a postdoc, two as a first author. He is currently working as a medical liaison for Onyx Pharmaceuticals.

Dawn Delfin enrolled in the Medicinal Chemistry and Pharmacognosy graduate program in fall 2002 and was a recipient of a Chemistry-Biology Interface (CBI) training grant, a fellowship from the National Organization for Black Chemists and Chemical Engineers, and a fellowship from the United Negro College Fund/Merck. Dawn’s work in my lab as a graduate student and during her short time as a postdoc resulted in the publication of nine papers in total, and she was the first author on two of these papers. Dawn now works as a postdoc in Jill Rafael-Fortney's lab in the Department of Molecular and Cellular Biochemistry at The Ohio State University and has three first author papers from that experience. She is currently looking for academic positions.

Manar Salem enrolled in the Medicinal Chemistry and Pharmacognosy graduate program at Ohio State in fall 2000, obtained a masters degree in this program in 2003, and earned a Ph.D. in Medicinal Chemistry and Pharmacognosy in 2005. During her time as a graduate student at OSU, she received the Jane Chen Graduate Fellowship in medicinal chemistry and pharmacognosy in both 2002 and 2003. Manar was awarded an OSU Presidential Fellowship in 2004 and also obtained the Benjamin Balshone Graduate Student Award from the OSU College of Pharmacy in the same year. Manar served as a Postdoctoral Researcher in the College of Pharmacy at OSU from 2005-2006. In 2006, she became an assistant professor of pharmacognosy on the Faculty of Pharmacy at Tanta University in Egypt. Manar’s work in my lab as a graduate student and during her brief time as a postdoc resulted in the publication of eleven papers in total, and she was the first author on four of these papers. A paper that she published in the Journal of Natural Products in 2006 focusing on the antiparasitic activity of compounds from a different desert plant she worked on was among the 10 most accessed articles in the journal that year. Manar joined the OSU Havener Eye Institute retina research lab in 2009. Just prior to her tragic death in August 2011, she made three separate presentations of her work at the annual American Society of Pharmacognosy meeting, the premier conference for natural products research.

Academic Advising

2002 - present , The Ohio State University.
2007 - present Pandharkar, Trupti, The Ohio State University College of Pharmacy.
2007 - present Richard, Julian, The Ohio State University College of Pharmacy.
2000 - 2005 Salem, Manar, The Ohio State University College of Pharmacy. Graduated 2005. Identification of Antikinetoplastid Compounds from Psorothamnus polydenius and P. arborescens
2005 - 2006 Nzimiro, Sandra, The Ohio State University College of Pharmacy. Graduated 2006. Mechanistic Studies of Pentamidine Analogs on Leishmania donovani Promastigotes
2001 - 2007 Delfin, Dawn, The Ohio State University College of Pharmacy. Graduated 2007. A Novel and Potent Antileishmanial Agent: In Silico Discovery, Biological Evaluation, and Analysis of its Structure-Activity Relationships
2002 - 2007 Yakovich, Adam, The Ohio State University College of Pharmacy. Graduated 2007. Old Targets and New Beginnings: A Multifaceted Approach to Combating Leishmaniasis, a Neglected Tropical Disease
2007 Manley, Joshua, The Ohio State University College of Pharmacy. Graduated 2007. Studies toward the Synthesis of Amidine, Methoxime and Amidoxime Dihydroquinolines as Antitrypanosomal Candidates
2004 - 2008 Latibeaudiere, Kirk, The Ohio State University College of Pharmacy. Graduated 2008. Regioisomers of the Dinitroaniline Scaffold: Exploring Tubulin Assembly Inhibition through Novel Antikinetoplastid Agents
2009 Hans, Renate, University of Cape Town. Graduated 2009.
2007 - 2012 He, Shanshan, The Ohio State University College of Pharmacy. Graduated 2012. Neglected Tropical Disease Chemotherapy: Mechanistic Characterization of Antitrypanosomal Dihydroquinolines and Development of a High Throughput Antileishmanial Screening Assay
2010 - 2012 Young, Jason, The Ohio State University College of Pharmacy. Graduated 2012. Synthesis of Allosteric Modulators for Nicotinic Acetylcholine Receptors
2012 Njogu, Peter, University of Cape Town. Graduated 2012.
 

Conferences

Mitra,A; Morrissette,N,S; Werbovetz,K,A; Sept,D. "Dinitroanilines Bind to Alpha-tubulin of Apicomplexan and Kinetoplastid Parasites." In Molecular Biology of the Cell. (November 2004). 295A-295A.

Yakovich,Adam; George,Tesmol; Johnsamuel,Jayaseharan; Delfin,Dawn; Dalton,James; Wu,Di; Phelps,Mitch; Werbovetz,Karl. "Evaluation of Novel Antileishmanial Antimitotic Agents." In American Journal of Tropical Medicine and Hygiene. (December 2005). 100-100.

Werbovetz,Karl; Salem,Manar; Mukherjee,Mitali; Zidan,Samia; Bahar,Mark; Fletcher,Joshua; Hassan,Nasir; Kinghorn,A,Douglas. "Identification of Antikinetoplastid Compounds from Plants." In American Journal of Tropical Medicine and Hygiene. (December 2005). 26-27.

Delfin,Dawn,A; Bhattacharjee,Apurba,K; Werbovetz,Karl,A. "Identification of Novel Antileishmanial Compounds through in Silico Pharmacophore Development and Database Searching." In Abstracts of Papers of the American Chemical Society. (August 2005). U2618-U2618.

Salem,M,M; Werbovetz,K,A. "Antiparasitic Compounds from Psorothamnus arborescens." In Abstracts of Papers of the American Chemical Society. (March 2005). U178-U178.

Ismail,Mohamed,A; Paliakov,Ekaterina,M; Boykin,David,W; Stephens,Chad,E; Werbovetz,Karl,A; Brun,Reto. "Efficient Synthesis and Anti-Protozoal Evaluation of 2,2 '-Bichalcophene Analogues of Furamidine." In Abstracts of Papers of the American Chemical Society. (March 2006). MEDI-360.

Werbovetz,Karl; Endeshaw,Molla; Morgan,Rachel; Li,Chenglong; Diraviyam,Karthikeyan; Sept,David. "Parasite Tubulin as a Drug Target." In American Journal of Tropical Medicine and Hygiene. (November 2007). 286-287.

Zhu,Xiaohua; Stephens,Chad; Kumar,Arvind; Sweat,Mark; Pandharkar,Trupti; Kyle,Dennis; Boykin,David; Werbovetz,Karl. "Reversed Amidines as Antileishmanial Candidates." In American Journal of Tropical Medicine and Hygiene. (December 2008). 159-159.

Reid,Carolyn; He,Shanshan; Patrick,Donald,A; Kokku,Premalatha; Fotie,Jean; Wenzler,Tanja; Brun,Reto; Tidwell,Richard,R; Werbovetz,Karl. "Dihydroquinolines with in Vitro and in Vivo Activity against African Trypanosomes." In American Journal of Tropical Medicine and Hygiene. (November 2010). 203-204.

Zhu,Xiaohua; Banerjee,Moloy; Farhat,Abdelbasset,A; Reid,Carolyn; Pandharkar,Trupti; Patrick,Donald,A; Tidwell,Richard,R; Wang,Michael; Kyle,Dennis; Boykin,David; Werbovetz,Karl. "Antileishmanial Activity of Novel Arylimidamides." In American Journal of Tropical Medicine and Hygiene. (November 2010). 71-71.

Collar,Catharine,J; Zhu,Xiaohua; Werbovetz,Karl; Boykin,David,W; Wilson,W,David. "Designing Treatments for Leishmaniasis: Employing Computational Tools to Examine Biological Affinity and Mechanisms of Arylimidamides." In Abstracts of Papers of the American Chemical Society. (March 2010). MEDI-77.

Chin, Y, Bahar, M, Keller, W, Werbovetz, K, Kinghorn, AD. "Compounds with Potential Antileishmanial Activity from Licorice (Glycerrhiza glabra)." 48th Annual Meeting of the American Society of Pharmacognosy, 2007. .

Salem, M, Werbovetz, K. "Natural Products as Antiparasitic Drugs." 36th Graduate Student Symposium in Medicinal Chemistry, 2003. .

Pandharkar, T, Boykin, D, Werbovetz, K.. "Understanding the Mechanism of Action of the Anti-leishmanial Arylimidamide DB766." American Society of Tropical Medicine and Hygiene 60th Annual Meeting, 2011. .

He, S, Drew, M, Werbovetz, K. "RNA Interference of Enzymes Involved in Parasite Antioxidant Defense Indicates the Novel Antitrypanosomal Compound OSU-40 Acts through Generation of Reactive Oxygen Species." Kinetoplastid Molecular Cell Biology Meeting, 2011. .

Fletcher, J, Doskotch, RW, Werbovetz, K, Kinghorn, AD. "Antileishmanial Bioactivity-guided Fractionation of Ficus elastica." 48th Annual Meeting of the American Society of Pharmacognosy, 2007. .

Delfín, D, Werbovetz, K. "Solid Phase Combinatorial Synthesis of Dinitroaniline Sulfonamides and their Evaluation for Antiparasitic Activity." 36th Graduate Student Symposium in Medicinal Chemistry, 2004. .

Delfín, D, Bhattacharjee, A, Yakovich, A, Werbovetz, K. "Activity of and Mechanistic Studies on a Novel Antileishmanial Agent Identified in Silico." Keystone Symposium - Drugs Against Protozoan Parasites, 2007. .

Bhattacharya, G, Werbovetz, K. "Synthesis of Substituted N-phenyl Acetamides as Candidate Inhibitors of Malarial Lactate Dehydrogenase." 34th Graduate Student Symposium in Medicinal Chemistry, 2001. .

Zhu, X, Pandharkar, T, Werbovetz, K.. "Identification of Antileishmanial Benzothiazoles Based on Hits from a High-throughput Promastigote Screen." American Society of Tropical Medicine and Hygiene 60th Annual Meeting, 2011. .

Yakovich, A, Mukherjee, M, Werbovetz, K. "High Throughput Screening as a Tool to Identify Novel Antileishmanial Compounds." Pharmaceutical Sciences World Congress (PSWC), 3rd Meeting, 2007. .

Werbovetz, K, Wu, D, George, T, Delfín, D, Yakovich, A, Kaiser, M, Brun, R, Dalton, J. "Activity, Metabolism, and Pharmacokinetics of Antikinetoplastid Antimitotic N1,N4-substituted 3,5-Dinitro Sulfanilamides." Keystone Symposium - Drugs Against Protozoan Parasites, 2005. .

Werbovetz, K, Varadhachary, A, Englund, P.. "A Fatty Acyl-CoA Synthetase from Trypanosoma brucei with a Preference for Myristate." Molecular Parasitology Meeting VII, 1996. .

Werbovetz, K, Sackett, D. "Purification, Characterization, and Drug Susceptibility of Tubulin from Leishmania." American Society of Tropical Medicine and Hygiene 46th Annual Meeting, 1997. .

Werbovetz, K, Miller, K, Macdonald, T, Pearson, R. "Cleavable Complex Formation in Leishmania chagasi Treated with Anilinoacridines." Third Annual Meeting of the NIAID Network of International Centers for Tropical Disease Research, 1994. .

Werbovetz, K, Havens, C, McCrary, G, Perfetto, S. "Cellular Effects of Leishmanial Tubulin Inhibitors on L. donovani." Molecular Parasitology Meeting X, 1999. .

Werbovetz, K, Englund, P. "Incorporation of [3H]Myristate into Trypanosoma brucei GPIs from [3H]Myristoyllyso Phosphatidylcholine Donor." Molecular Parasitology Meeting V, 1994. .

Werbovetz, K, Delfin, Bhattacharya, G, Salem, M, Sackett, D, Gerena, L, Lopez-Sanchez, M, Rattendi, D, Bacchi, C. "Potent and Selective Antimicrotubule Activity of the Synthetic Dinitroaniline Sulfonamide GB-II-5 against Kinetoplastid Parasites." Molecular Parasitology Meeting XIII, 2002. .

Werbovetz, K, Brendle, J, Sackett, D. "Susceptibility of Leishmanial Tubulin to Microtubule Inhibitors." 1st COST-B9 Congress on Antiprotozoal Chemotherapy, 1998. .

Werbovetz, K, Brendle, J, Mendez, S, Alunda, J, Sackett, D. "Leishmanial Tubulin as a Drug Target: Lead Compounds Identified and Challenges Encountered." 2nd COST-B9 Congress on Antiprotozoal Chemotherapy, 1999. .

Werbovetz, K, Bhattacharya, G, Salem, M, Barszcz, T, Delfin, D. "Selective Antimitotic Agents Against Kinetoplastid Parasites." American Society of Tropical Medicine and Hygiene 52nd Annual Meeting, 2003. .

Werbovetz, K, Bhattacharjee, A. "Comparison of Mammalian and Leishmanial Beta Tubulin in the “Colchicine Binding” Region: Implications for Antiparasitic Drug Discovery." Molecular Parasitology Meeting XI, 2000. .

Werbovetz, K, Barszcz, T, Salem, Bakunova, S, Bakunova, S, Tidwell, R. "New Benzofuran-containing Diamidines with Improved Antileishmanial Activity Compared to Pentamidine." American Society of Tropical Medicine and Hygiene 52nd Annual Meeting, 2003. .

Werbovetz, K, Barszcz, T, Nzimiro, S, Wenzler, T, Brun, R, Arafa, R, Ismail, M, Boykin, D. "Linear and Near-linear Diamidines with Potent Antileishmanial Activity." Keystone Symposium – Drugs Against Protozoan Parasites, 2007. .

Werbovetz, K, Bacchi, C, Englund, P. "Comparison of Myristate and Myristoyllyso Phosphatidylcholine as Myristate Donors for Trypanosoma brucei GPIs." Second International Congress of the International Society for the Study of Fatty Acids and Lipids, 1995. .

Morgan, R, Werbovetz, K. "Screening against Leishmanial Tubulin to Identify Novel Antileishmanial Compounds." Keystone Symposium – Drugs Against Protozoan Parasites, 2007. .

 

Degrees

1988 B.S., State University of New York at Binghamton

1993 Ph.D., University of Virginia

 

Editorial Activities

2001 - 2008 Mini-Reviews in Medicinal Chemistry
2005 - present Bioorganic and Medicinal Chemistry
2005 - present Bioorganic and Medicinal Chemistry Letters
2005 - present Journal of Medicinal Chemistry
2005 - 2006 Microbiology and Immunology Study Section, American Heart Association
2005 - 2008 Journal of Natural Products
2006 - present Journal of Antimicrobial Chemotherapy
2006 - present European Journal of Medicinal Chemistry
2007 - present Acta Tropica
2007 - present Antimicrobial Agents and Chemotherapy
2008 - present Biochemistry
2008 - present ChemMedChem
2009 - present DoD Antiparasitic Drug Research Program, Military Infectious Diseases Research Program
2009 - present PLoS Neglected Tropical Diseases
2009 Infectious Diseases and Microbiology IRG (DDR Study Section) Challenge Grant review
2010 - present MedChemComm
2010 - present Parasitology
2010 NIH SMARTT (Science Moving towArd Research Translation and Therapy) program special emphasis panel
2011 King Abdulaziz City for Science and Technology Research Competition, American Association for the Advancement of Science Research Competitiveness Program
2011 NIH Tropical Medicine Research Centers special emphasis panel
2012 - present Non-HIV Anti-Infective Therapeutics SBIR-STTR Study Section (ZRG1-IDM-U)
 

Honors

2005 Distinguished Teaching Award. Bachelor of Science in the Pharmaceutical Sciences program, College of Pharmacy.
 

Journal Articles

Huber,S,K; Werbovetz,K,A; Obaza-Nutaitis,J; Lehnert,E,K; Macdonald,T,L. "Tubulin Binding of Conformationally Restricted Bis-aryl Compounds." Bioorganic and Medicinal Chemistry Letters. Vol. 1, no. 5. (January 1991.): 243-246.

Werbovetz, K, A; Lehnert, E, K; Macdonald, T, L; Pearson, R D. "Cytotoxicity of acridine compounds for Leishmania promastigotes in vitro.." Antimicrobial agents and chemotherapy. Vol. 36, no. 2. (January 1992.): 495-7.

Werbovetz,K,A; Lehnert,E,K; Macdonald,T,L; Pearson,R,D. "Cytotoxicity of Acridine Compounds for Leishmania Promastigotes in Vitro." Antimicrobial Agents and Chemotherapy. Vol. 36, no. 2. (February 1992.): 495-497.

Werbovetz,K,A; Jeronimo,S,M; Macdonald,T,L; Pearson,R,D. "Treatment of Leishmaniansis and Trypanosomiasis." Current Opinion in Infectious Disease. Vol. 5, no. 6. (December 1992.): 840-848.

Werbovetz,K,A; Macdonald,T,L. "On the Mechanism of Arylamine-DNA Adduct Formation." Bioorganic and Medicinal Chemistry Letters. Vol. 4, no. 19. (October 1994.): 2323-2326.

Doering,T,L; Lu,T,B; Werbovetz,K,A; Gokel,G,W; Hart,G,W; Gordon,J,I; Englund,P,T. "Toxicity of Myristic Acid Analogs Toward African Trypanosomes." Proceedings of the National Academy of Sciences of the United States of America. Vol. 91, no. 21. (October 1994.): 9735-9739.

Werbovetz,K,A; Spoors,P,G; Pearson,R,D; MACDONALD,T,L. "Cleavable Complex Formation in Leishmania chagasi Treated with Anilinoacridines." Molecular and Biochemical Parasitology. Vol. 65, no. 1. (May 1994.): 1-10.

Werbovetz, K, A; Spoors, P, G; Pearson, R, D; Macdonald, T L. "Cleavable complex formation in Leishmania chagasi treated with anilinoacridines.." Molecular and biochemical parasitology. Vol. 65, no. 1. (January 1994.): 1-10.

Doering, T, L; Lu, T; Werbovetz, K, A; Gokel, G, W; Hart, G, W; Gordon, J, I; Englund, P T. "Toxicity of myristic acid analogs toward African trypanosomes.." Proceedings of the National Academy of Sciences of the United States of America. Vol. 91, no. 21. (January 1994.): 9735-9.

Werbovetz,K,A; Bacchi,C,J; Englund,P,T. "Trypanocidal Analogs of Myristate and Myristoyllysophosphatidylcholine." Molecular and Biochemical Parasitology. Vol. 81, no. 1. (October 1996.): 115-118.

Tepe,J,J; Madalengoitia,J,S; Slunt,K,M; Werbovetz,K,A; Spoors,P,G; MACDONALD,T,L. "Inhibition of DNA Topoisomerase II by Azaelliptitoxins Functionalized in the Variable Substituent Domain." Journal of Medicinal Chemistry. Vol. 39, no. 11. (May 1996.): 2188-2196.

Buxbaum,L,U; Milne,K,G; Werbovetz,K,A; Englund,P,T. "Myristate Exchange on the Trypanosoma brucei Variant Surface Glycoprotein." Proceedings of the National Academy of Sciences of the United States of America. Vol. 93, no. 3. (February 1996.): 1178-1183.

Werbovetz,K,A; Englund,P,T. "Lipid Metabolism in Trypanosoma brucei: Utilization of Myristate and Myristoyllysophosphatidylcholine for Myristoylation of Glycosyl Phosphatidylinositols." Biochemical Journal. Vol. 318, (September 1996.): 575-581.

Buxbaum, L, U; Milne, K, G; Werbovetz, K, A; Englund, P T. "Myristate exchange on the Trypanosoma brucei variant surface glycoprotein.." Proceedings of the National Academy of Sciences of the United States of America. Vol. 93, no. 3. (January 1996.): 1178-83.

Werbovetz, K, A; Englund, P T. "Lipid metabolism in Trypanosoma brucei: utilization of myristate and myristoyllysophosphatidylcholine for myristoylation of glycosyl phosphatidylinositols.." The Biochemical journal. Vol. 318 ( Pt 2), (January 1996.): 575-81.

Werbovetz, K, A; Bacchi, C, J; Englund, P T. "Trypanocidal analogs of myristate and myristoyllysophosphatidylcholine.." Molecular and biochemical parasitology. Vol. 81, no. 1. (January 1996.): 115-8.

Werbovetz,K,A; Englund,P,T. "Glycosyl Phosphatidylinositol Myristoylation in African Trypanosomes." Molecular and Biochemical Parasitology. Vol. 85, no. 1. (March 1997.): 1-7.

Madalengoitia, J, S; Tepe, J, J; Werbovetz, K, A; Lehnert, E, K; Macdonald, T L. "Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues.." Bioorganic & medicinal chemistry. Vol. 5, no. 9. (January 1997.): 1807-15.

Werbovetz, K, A; Englund, P T. "Glycosyl phosphatidylinositol myristoylation in African trypanosomes.." Molecular and biochemical parasitology. Vol. 85, no. 1. (January 1997.): 1-7.

Madalengoitia,J,S; Tepe,J,J; Werbovetz,K,A; Lehnert,E,K; MACDONALD,T,L. "Structure-activity Relationship for DNA Topoisomerase II-induced DNA Cleavage by Azatoxin Analogues." Bioorganic and Medicinal Chemistry. Vol. 5, no. 9. (September 1997.): 1807-1815.

Pitzer,K,K; Werbovetz,K,A; Brendle,J,J; Scovill,J,P. "Synthesis and Biological Evaluation of 4-Chloro-3,5-dinitrobenzotrifluoride Analogues as Antileishmanial Agents." Journal of Medicinal Chemistry. Vol. 41, no. 24. (November 1998.): 4885-4889.

Pitzer, K, K; Werbovetz, K, A; Brendle, J, J; Scovill, J P. "Synthesis and biological evaluation of 4-chloro-3, 5-dinitrobenzotrifluoride analogues as antileishmanial agents.." Journal of medicinal chemistry. Vol. 41, no. 24. (January 1998.): 4885-9.

Werbovetz,K,A; Brendle,J,J; Sackett,D,L. "Purification, Characterization, and Drug Susceptibility of Tubulin from Leishmania." Molecular and Biochemical Parasitology. Vol. 98, no. 1. (January 1999.): 53-65.

Werbovetz, K, A; Brendle, J, J; Sackett, D L. "Purification, characterization, and drug susceptibility of tubulin from Leishmania.." Molecular and biochemical parasitology. Vol. 98, no. 1. (January 1999.): 53-65.

Havens, C, G; Bryant, N; Asher, L; Lamoreaux, L; Perfetto, S; Brendle, J, J; Werbovetz, K A. "Cellular effects of leishmanial tubulin inhibitors on L. donovani.." Molecular and biochemical parasitology. Vol. 110, no. 2. (January 2000.): 223-36.

Werbovetz, K, A; Bhattacharjee, A, K; Brendle, J, J; Scovill, J P. "Analysis of stereoelectronic properties of camptothecin analogues in relation to biological activity.." Bioorganic & medicinal chemistry. Vol. 8, no. 7. (January 2000.): 1741-7.

Werbovetz,K,A; Bhattacharjee,A,K; Brendle,J,J; Scovill,J,P. "Analysis of Stereoelectronic Properties of Camptothecin Analogues in Relation to Biological Activity." Bioorganic and Medicinal Chemistry. Vol. 8, no. 7. (July 2000.): 1741-1747.

Werbovetz,K,A. "Target-based Drug Discovery for Malaria, Leishmaniasis, and Trypanosomiasis." Current Medicinal Chemistry. Vol. 7, no. 8. (August 2000.): 835-860.

Werbovetz, K A. "Target-based drug discovery for malaria, leishmaniasis, and trypanosomiasis.." Current medicinal chemistry. Vol. 7, no. 8. (January 2000.): 835-60.

Havens,C,G; Bryant,N; Asher,L; Lamoreaux,L; Perfetto,S; Brendle,J,J; Werbovetz,K,A. "Cellular Effects of Leishmanial Tubulin Inhibitors on L. donovani." Molecular and Biochemical Parasitology. Vol. 110, no. 2. (October 2000.): 223-236.

Bhattacharya, Gautam; Salem, Manar, M; Werbovetz, Karl A. "Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin.." Bioorganic & medicinal chemistry letters. Vol. 12, no. 17. (January 2002.): 2395-8.

Bhattacharya,G; Salem,M,M; Werbovetz,K,A. "Antileishmanial Dinitroaniline Sulfonamides with Activity against Parasite Tubulin." Bioorganic and Medicinal Chemistry Letters. Vol. 12, no. 17. (September 2002.): 2395-2398.

Brendle, James, J; Outlaw, Abram; Kumar, Arvind; Boykin, David, W; Patrick, Donald, A; Tidwell, Richard, R; Werbovetz, Karl A. "Antileishmanial activities of several classes of aromatic dications.." Antimicrobial agents and chemotherapy. Vol. 46, no. 3. (January 2002.): 797-807.

Bhattacharjee, Apurba, K; Skanchy, David, J; Jennings, Barton; Hudson, Thomas, H; Brendle, James, J; Werbovetz, Karl A. "Analysis of stereoelectronic properties, mechanism of action and pharmacophore of synthetic indolo[2,1-b]quinazoline-6,12-dione derivatives in relation to antileishmanial activity using quantum chemical, cyclic voltammetry and 3-D-QSAR CATALYST." Bioorganic & medicinal chemistry. Vol. 10, no. 6. (January 2002.): 1979-89.

Werbovetz, Karl A. "Promising therapeutic targets for antileishmanial drugs.." Expert opinion on therapeutic targets. Vol. 6, no. 4. (January 2002.): 407-22.

Werbovetz, Karl A. "Tubulin as an antiprotozoal drug target.." Mini reviews in medicinal chemistry. Vol. 2, no. 6. (January 2002.): 519-29.

Bhattacharjee,A,K; Skanchy,D,J; Jennings,B; Hudson,T,H; Brendle,J,J; Werbovetz,K,A. "Analysis of Stereoelectronic Properties, Mechanism of Action and Pharmacophore of Synthetic indolo[2,1-b]quinazoline-6,12-dione Derivatives in Relation to Antileishmanial Activity using Quantum Chemical, Cyclic Voltammetry and 3-D-QSAR CATALYST Procedures." Bioorganic and Medicinal Chemistry. Vol. 10, no. 6. (June 2002.): 1979-1989.

Werbovetz,K,A. "Promising Therapeutic Targets for Antileishmanial Drugs." Expert Opinion on Therapeutic Targets. Vol. 6, no. 4. (August 2002.): 407-422.

Werbovetz,Karl,A. "Tubulin as an Antiprotozoal Drug Target." Mini Reviews in Medicinal Chemistry. Vol. 2, no. 6. (December 2002.): 519-529.

Brendle,J,J; Outlaw,A; Kumar,A; Boykin,D,W; Patrick,D,A; Tidwell,R,R; Werbovetz,K,A. "Antileishmanial Activities of Several Classes of Aromatic Dications." Antimicrobial Agents and Chemotherapy. Vol. 46, no. 3. (March 2002.): 797-807.

Stephens,C,E; Brun,R; Salem,M,M; Werbovetz,K,A; Tanious,F; Wilson,W,D; Boykin,D,W. "The Activity of Diguanidino and 'Reversed' Diamidino 2,5-Diarylfurans versus Trypanosoma cruzi and Leishmania donovani." Bioorganic and Medicinal Chemistry Letters. Vol. 13, no. 12. (June 2003.): 2065-2069.

Werbovetz,K,A; Sackett,D,L; Delfin,D; Bhattacharya,G; Salem,M; Obrzut,T; Rattendi,D; Bacchi,C. "Selective Antimicrotubule Activity of N1-phenyl-3,5-dinitro-N4,N4-di-n-propylsulfanilamide (GB-II-5) against Kinetoplastid Parasites." Molecular Pharmacology. Vol. 64, no. 6. (December 2003.): 1325-1333.

Hua, Duy, H; Tamura, Masafumi; Egi, Masahiro; Werbovetz, Karl; Delfin, Dawn; Salem, Manar; Chiang, Peter K. "Antiprotozoal activities of symmetrical bishydroxamic acids.." Bioorganic & medicinal chemistry. Vol. 11, no. 20. (January 2003.): 4357-61.

Werbovetz, Karl, A; Sackett, Dan, L; Delfin, Dawn; Bhattacharya, Gautam; Salem, Manar; Obrzut, Tomasz; Rattendi, Donna; Bacchi, Cyrus. "Selective antimicrotubule activity of N1-phenyl-3,5-dinitro-N4,N4-di-n-propylsulfanilamide (GB-II-5) against kinetoplastid parasites.." Molecular pharmacology. Vol. 64, no. 6. (January 2003.): 1325-33.

Stephens, Chad, E; Brun, Reto; Salem, Manar, M; Werbovetz, Karl, A; Tanious, Farial; Wilson, W David; Boykin, David W. "The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.." Bioorganic & medicinal chemistry letters. Vol. 13, no. 12. (January 2003.): 2065-9.

Hua,D,H; Tamura,M; Egi,M; Werbovetz,K; Delfin,D; Salem,M; Chiang,P,K. "Antiprotozoal Activities of Symmetrical Bishydroxamic Acids." Bioorganic and Medicinal Chemistry. Vol. 11, no. 20. (October 2003.): 4357-4361.

Bhattacharya,G; Herman,J; Delfin,D; Salem,M,M; Barszcz,T; Mollet,M; Riccio,G; Brun,R; Werbovetz,K,A. "Synthesis and Antitubulin Activity of N-1- and N-4-substituted 3,5-dinitro Sulfanilamides against African Trypanosomes and Leishmania." Journal of Medicinal Chemistry. Vol. 47, no. 7. (March 2004.): 1823-1832.

Arafa,R,K; Brun,R; Werbovetz,K,A; Tanious,F,A; Wilson,W,D; Boykin,D,W. "Synthesis of Dicationic 2,5-Diarylpyrroles." Heterocyclic Communications. Vol. 10, no. 6. (January 2004.): 423-428.

Jiang,D,W; Werbovetz,K,A; Varadhachary,A; Cole,R,N; Englund,P,T. "Purification and Identification of a Fatty acyl-CoA Synthetase from Trypanosoma brucei." Molecular and Biochemical Parasitology. Vol. 135, no. 1. (May 2004.): 149-152.

Cottrell, Denise, M; Capers, Jeffrey; Salem, Manar, M; DeLuca-Fradley, Kate; Croft, Simon, L; Werbovetz, Karl A. "Antikinetoplastid activity of 3-aryl-5-thiocyanatomethyl-1,2,4-oxadiazoles.." Bioorganic & medicinal chemistry. Vol. 12, no. 11. (January 2004.): 2815-24.

Bhattacharya, Gautam; Herman, Johnathan; Delfin, Dawn; Salem, Manar, M; Barszcz, Todd; Mollet, Mike; Riccio, Guy; Brun, Reto; Werbovetz, Karl A. "Synthesis and antitubulin activity of N1- and N4-substituted 3,5-dinitro sulfanilamides against African trypanosomes and Leishmania.." Journal of medicinal chemistry. Vol. 47, no. 7. (January 2004.): 1823-32.

Jiang, David, W; Werbovetz, Karl, A; Varadhachary, Atul; Cole, Robert, N; Englund, Paul T. "Purification and identification of a fatty acyl-CoA synthetase from Trypanosoma brucei.." Molecular and biochemical parasitology. Vol. 135, no. 1. (January 2004.): 149-52.

Cottrell,D,M; Capers,J; Salem,M,M; DeLuca-Fradley,K; Croft,S,L; Werbovetz,K,A. "Antikinetoplastid Activity of 3-Aryl-5-thiocyanatomethyl-1,2,4-oxadiazoles." Bioorganic and Medicinal Chemistry. Vol. 12, no. 11. (June 2004.): 2815-2824.

Salem,M,M; Werbovetz,K,A. "Antiprotozoal Compounds from Psorothamnus polydenius." Journal of Natural Products. Vol. 68, no. 1. (January 2005.): 108-111.

Salem, Manar, M; Werbovetz, Karl A. "Antiprotozoal compounds from Psorothamnus polydenius.." Journal of natural products. Vol. 68, no. 1. (January 2005.): 108-11.

Li, Pui-Kai; Xiao, Zili; Hu, Zhigen; Pandit, Bulbul; Sun, Yanjun; Sackett, Dan, L; Werbovetz, Karl; Lewis, Andrew; Johnsamuel, Jayasekar. "Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.." Bioorganic & medicinal chemistry letters. Vol. 15, no. 24. (January 2005.): 5382-5.

Li,P,K; Xiao,Z,L; Hu,Z,G; Pandit,B; Sun,Y,J; Sackett,D,L; Werbovetz,K; Lewis,A; Johnsamuel,J. "Conformationally Restricted Analogs of Combretastatin A-4 Derived from SU5416." Bioorganic and Medicinal Chemistry Letters. Vol. 15, no. 24. (December 2005.): 5382-5385.

Bhattacharya,G; Gerena,L; Jiang,S,P; Werbovetz,K,A. "Activity of Amidine-containing Diphenylureas against P. falciparum." Letters in Drug Design and Discovery. Vol. 2, no. 2. (March 2005.): 162-164.

Werbovetz, Karl. "Diamidines as antitrypanosomal, antileishmanial and antimalarial agents.." Current opinion in investigational drugs (London, England : 2000). Vol. 7, no. 2. (January 2006.): 147-57.

Yakovich,Adam,J; Ragone,Frank,L; Alfonzo,Juan,D; Sackett,Dan,L; Werbovetz,Karl,A. "Leishmania tarentolae: Purification and Characterization of Tubulin and its Suitability for Antileishmanial Drug Screening." Experimental Parasitology. Vol. 114, no. 4. (December 2006.): 289-296.

Wu, Di; George, Tesmol, G; Hurh, Eunju; Werbovetz, Karl, A; Dalton, James T. "Pre-systemic metabolism prevents in vivo antikinetoplastid activity of N1,N4-substituted 3,5-dinitro sulfanilamide, GB-II-150.." Life sciences. Vol. 79, no. 11. (January 2006.): 1081-93.

Salem,Manar,M; Werbovetz,Karl,A. "Natural Products from Plants as Drug Candidates and Lead Compounds Against Leishmaniasis and Trypanosomiasis." Current Medicinal Chemistry. Vol. 13, no. 21. (September 2006.): 2571-2598.

Salem, Manar, M; Werbovetz, Karl A. "Natural products from plants as drug candidates and lead compounds against leishmaniasis and trypanosomiasis.." Current medicinal chemistry. Vol. 13, no. 21. (January 2006.): 2571-98.

Salem, Manar, M; Werbovetz, Karl A. "Isoflavonoids and other compounds from Psorothamnus arborescens with antiprotozoal activities.." Journal of natural products. Vol. 69, no. 1. (January 2006.): 43-9.

Yakovich, Adam, J; Ragone, Frank, L; Alfonzo, Juan, D; Sackett, Dan, L; Werbovetz, Karl A. "Leishmania tarentolae: purification and characterization of tubulin and its suitability for antileishmanial drug screening.." Experimental parasitology. Vol. 114, no. 4. (January 2006.): 289-96.

Li,P,K; Pandit,B; Sackett,D,L; Hu,Z,G; Zink,J; Zhi,J,D; Freeman,D; Robey,R,W; Werbovetz,K; Lewis,A; Li,C,L. "A Thalidomide Analogue with in Vitro Antiproliferative, Antimitotic, and Microtubule-stabilizing Activities." Molecular Cancer Therapeutics. Vol. 5, no. 2. (February 2006.): 450-456.

Das,Umashankar; Gul,H,Inci; Alcorn,Jane; Shrivastav,Anuraag; George,Theresa; Sharma,Rajendra,K; Nienaber,Kurt,H; De Clercq,Erik; Balzarini,Jan; Kawase,Masami; Kan,Noriyuki; Tanaka,Torn; Tani,Satoru; Werbovetz,Karl,A; Yakovich,Adam,J; Manavathu,Elias,K; Stables,James,P; Dimmock,Jonathan,R. "Cytotoxic 5-Aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes Mounted on Alicyclic Scaffolds." European Journal of Medicinal Chemistry. Vol. 41, no. 5. (May 2006.): 577-585.

Werbovetz,K. "Diamidines as Antitrypanosomal, Antileishmanial and Antimalarial Agents." Current Opinion in Investigational Drugs. Vol. 7, no. 2. (February 2006.): 147-157.

George,Tesmol,G; Johnsamuel,Jayaseharan; Delfin,Dawn,A; Yakovich,Adam; Mukherjee,Mitali; Phelps,Mitch,A; Dalton,James,T; Sackett,Dan,L; Kaiser,Marcel; Brun,Reto; Werbovetz,Karl,A. "Antikinetoplastid Antimitotic Activity and Metabolic Stability of Dinitroaniline Sulfonamides and Benzamides." Bioorganic and Medicinal Chemistry. Vol. 14, no. 16. (August 2006.): 5699-5710.

Salem,M,M; Werbovetz,K,A. "Isoflavonoids and Other Compounds from Psorothamnus arborescens with Antiprotozoal Activities." Journal of Natural Products. Vol. 69, no. 1. (January 2006.): 43-49.

George, Tesmol, G; Johnsamuel, Jayaseharan; Delfin, Dawn, A; Yakovich, Adam; Mukherjee, Mitali; Phelps, Mitch, A; Dalton, James, T; Sackett, Dan, L; Kaiser, Marcel; Brun, Reto; Werbovetz, Karl A. "Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides.." Bioorganic & medicinal chemistry. Vol. 14, no. 16. (January 2006.): 5699-710.

Delfin, Dawn, A; Bhattacharjee, Apurba, K; Yakovich, Adam, J; Werbovetz, Karl A. "Activity of and initial mechanistic studies on a novel antileishmanial agent identified through in silico pharmacophore development and database searching.." Journal of medicinal chemistry. Vol. 49, no. 14. (January 2006.): 4196-207.

Das, Umashankar; Gul, H Inci; Alcorn, Jane; Shrivastav, Anuraag; George, Theresa; Sharma, Rajendra, K; Nienaber, Kurt, H; De Clercq, Erik; Balzarini, Jan; Kawase, Masami; Kan, Noriyuki; Tanaka, Toru; Tani, Satoru; Werbovetz, Karl, A; Yakovich, Adam, J; Manavathu, Elias, K; Stables, James, P; Dimmock, Jonathan R. "Cytotoxic 5-aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes mounted on alicyclic scaffolds.." European journal of medicinal chemistry. Vol. 41, no. 5. (January 2006.): 577-85.

Wu,Di; George,Tesmol,G; Hurh,Eunju; Werbovetz,Karl,A; Dalton,James,T. "Pre-systemic Metabolism Prevents in Vivo Antikinetoplastid Activity of N1, N4-substituted-3,5 Dinitro Sulfanilamide, GB-II-150." Life Sciences. Vol. 79, no. 11. (August 2006.): 1081-1093.

Li, Pui-Kai; Pandit, Bulbul; Sackett, Dan, L; Hu, Zhigen; Zink, Jennifer; Zhi, Jiandong; Freeman, Dena; Robey, Robert, W; Werbovetz, Karl; Lewis, Andrew; Li, Chenglong. "A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities.." Molecular cancer therapeutics. Vol. 5, no. 2. (January 2006.): 450-6.

Delfin,Dawn,A; Bhattacharjee,Apurba,K; Yakovich,Adam,J; Werbovetz,Karl,A. "Activity of and Initial Mechanistic Studies on a Novel Antileishmanial Agent Identified through in Silico Pharmacophore Development and Database Searching." Journal of Medicinal Chemistry. Vol. 49, no. 14. (July 2006.): 4196-4207.

Bakunova,Svetlana,M; Bakunov,Stanislav,A; Wenzler,Tanja; Barszcz,Todd; Werbovetz,Karl,A; Brun,Reto; Hall,James,Edwin; Tidwell,Richard,R. "Synthesis and in Vitro Antiprotozoal Activity of Bisbenzofuran Cations." Journal of Medicinal Chemistry. Vol. 50, no. 23. (November 2007.): 5807-5823.

George, Tesmol, G; Endeshaw, Molla, M; Morgan, Rachel, E; Mahasenan, Kiran, V; Delfin, Dawn, A; Mukherjee, Mitali, S; Yakovich, Adam, J; Fotie, Jean; Li, Chenglong; Werbovetz, Karl A. "Synthesis, biological evaluation, and molecular modeling of 3,5-substituted-N1-phenyl-N4,N4-di-n-butylsulfanilamides as antikinetoplastid antimicrotubule agents.." Bioorganic & medicinal chemistry. Vol. 15, no. 18. (January 2007.): 6071-9.

Gutteridge, C, E; Vo, J, V; Tillett, C, B; Vigilante, J, A; Dettmer, J, R; Patterson, S, L; Werbovetz, K, A; Capers, J; Nichols, D, A; Bhattacharjee, A, K; Gerena, L. "Antileishmanial and antimalarial chalcones: synthesis, efficacy and cytotoxicity of pyridinyl and naphthalenyl analogs.." Medicinal chemistry (Sh?ariqah, United Arab Emirates). Vol. 3, no. 2. (January 2007.): 115-9.

Gonzalez, J; Stephens, C; Wenzler, T; Brun, R; Tanious, F; Wilson, W; Barszcz, T; Werbovetz, K; Boykin, D. "Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes." Eur. J. Med. Chem. (January 2007.): -.

Gutteridge,C,E; Vo,J,V; Tillett,C,B; Vigilante,J,A; Dettmer,J,R; Patterson,S,L; Werbovetz,K,A; Capers,J; Nichols,D,A; Bhattacharjee,A,K; Gerena,L. "Antileishmanial and Antimalarial Chalcones: Synthesis, Efficacy and Cytotoxicity of Pyridinyl and Naphthalenyl Analogs." Medicinal Chemistry. Vol. 3, no. 2. (March 2007.): 115-119.

George,Tesmol,G; Endeshaw,Molla,M; Morgan,Rachel,E; Mahasenan,Kiran,V; Delfin,Dawn,A; Mukherjee,Mitali,S; Yakovich,Adam,J; Fotie,Jean; Li,Chenglong; Werbovetz,Karl,A. "Synthesis, Biological Evaluation, and Molecular Modeling of 3,5-Substituted-N-1-phenyl-N-4,N-4-di-n-butylsulfanilamides as Antikinetoplastid Antimicrotubule Agents." Bioorganic and Medicinal Chemistry. Vol. 15, no. 18. (September 2007.): 6071-6079.

Bakunova, S; Bakunov, S; Wenzler, T; Barszcz, T; Werbovetz, K; Brun, R; Hall, J; Tidwell, R. "Synthesis and In Vitro Antiprotozoal Activity of Bisbenzofuran Cations." J. Med. Chem. (January 2007.): -.

Gonzalez,Jose,L; Stephens,Chad,E; Wenzler,Tanja; Brun,Reto; Tanious,Farial,A; Wilson,W,David; Barszcz,Todd; Werbovetz,Karl,A; Boykin,David,W. "Synthesis and Antiparasitic Evaluation of Bis-2,5-[4-guanidinophenyl]thiophenes." European Journal of Medicinal Chemistry. Vol. 42, no. 4. (April 2007.): 552-557.

Morgan,R,E; Werbovetz,K,A. "Selective Lead Compounds against Kinetoplastid Tubulin." Drug Targets in Kinetoplastid Parasites. Vol. 625, (January 2008.): 33-47.

Werbovetz, Karl A.. "Book review of “Leishmania: After the Genome”." ChemMedChem. Vol. 3, (August 2008.): 1278-1279.

Morgan,Rachel,E; Ahn,Sunnoo; Nzimiro,Sandra; Fotie,Jean; Phelps,Mitch,A; Cotrill,Jeffrey; Yakovich,Adam,J; Sackett,Dan,L; Dalton,James,T; Werbovetz,Karl,A. "Inhibitors of Tubulin Assembly Identified through Screening a Compound Library." Chemical Biology and Drug Design. Vol. 72, no. 6. (December 2008.): 513-524.

Joshi,Mandar,S; Bauer,John,A; Werbovetz,Karl,A; Barszcz,Todd; Patil,Popat,N. "Pharmacological and Biological Screening of Ascorbigen: Protection against Glucose-induced Endothelial Cell Toxicity." Phytotherapy Research. Vol. 22, no. 12. (December 2008.): 1581-1586.

Rosypal,Alexa,C; Werbovetz,Karl,A; Salem,Manar; Stephens,Chad,E; Kumar,Arvind; Boykin,David,W; Hall,James,E; Tidwell,Richard,R. "Inhibition by Dications of in Vitro Growth of Leishmania major and Leishmania tropica: Causative Agents of Old World Cutaneous Leishmaniasis." Journal of Parasitology. Vol. 94, no. 3. (June 2008.): 743-749.

Bakunov,Stanislav,A; Bakunova,Svetlana,M; Wenzler,Tanja; Barszcz,Todd; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Synthesis and Antiprotozoal Activity of Cationic 2-Phenylbenzofurans." Journal of Medicinal Chemistry. Vol. 51, no. 21. (November 2008.): 6927-6944.

Turabekova,M,A; Vinogradova,V,I; Rasulev,B,F; Levkovich,M,G; Werbovetz,K; Capers,J; Abdullaev,N,D. "Antiparasitic Activity of Certain Isoquinoline Alkaloids and their Hypothetical Complexes with Oligonucleotides." Chemistry of Natural Compounds. Vol. 44, no. 3. (May 2008.): 341-345.

George,Tesmol,G; Richard,Julian; Barszcz,Todd; Capers,Jeffrey; Werbovetz,Karl,A. "Flavylium Salts as Precursors of Biologically Active Chalcones." Letters in Drug Design and Discovery. Vol. 5, no. 1. (January 2008.): 69-73.

Hu,Laixing; Arafa,Reem,K; Ismail,Mohamed,A; Wenzler,Tanja; Brun,Reto; Munde,Manoj; Wilson,W,David; Nzimiro,Sandra; Samyesudhas,Serene; Werbovetz,Karl,A; Boykin,David,W. "Azaterphenyl Diamidines as Antileishmanial Agents." Bioorganic and Medicinal Chemistry Letters. Vol. 18, no. 1. (January 2008.): 247-251.

Delfin,Dawn,A; Morgan,Rachel,E; Zhu,Xiaohua; Werbovetz,Karl,A. "Redox-active Dinitrodiphenylthioethers against Leishmania: Synthesis, Structure-activity Relationships and Mechanism of Action Studies." Bioorganic and Medicinal Chemistry. Vol. 17, no. 2. (January 2009.): 820-829.

Bakunova,Svetlana,M; Bakunov,Stanislav,A; Wenzler,Tanja; Barszcz,Todd; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Synthesis and Antiprotozoal Activity of Pyridyl Analogues of Pentamidine." Journal of Medicinal Chemistry. Vol. 52, no. 15. (August 2009.): 4657-4667.

Patrick,Donald,A; Bakunov,Stanislav,A; Bakunova,Svetlana,M; Kumar,E,VKSuresh; Chen,Heidi; Jones,Susan,Kilgore; Wenzler,Tanja; Barzczc,Todd; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Synthesis and Antiprotozoal Activities of Dicationic Bis(phenoxymethyl)benzenes, Bis(phenoxymethyl)naphthalenes, and Bis(benzyloxy)naphthalenes." European Journal of Medicinal Chemistry. Vol. 44, no. 9. (September 2009.): 3543-3551.

Wasan,Kishor,M; Wasan,Ellen,K; Gershkovich,Pavel; Zhu,Xiaohua; Tidwell,Richard,R; Werbovetz,Karl,A; Clement,John,G; Thornton,Sheila,J. "Highly Effective Oral Amphotericin B Formulation against Murine Visceral Leishmaniasis." Journal of Infectious Diseases. Vol. 200, no. 3. (August 2009.): 357-360.

Bakunova,Svetlana,M; Bakunov,Stanislav,A; Patrick,Donald,A; Kumar,E,VKSuresh; Ohemeng,Kwasi,A; Bridges,Arlene,S; Wenzler,Tanja; Barszcz,Todd; Jones,Susan,Kilgore; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Structure-Activity Study of Pentamidine Analogues as Antiprotozoal Agents." Journal of Medicinal Chemistry. Vol. 52, no. 7. (April 2009.): 2016-2035.

Bakunov,Stanislav,A; Bakunova,Svetlana,M; Bridges,Arlene,S; Wenzler,Tanja; Barszcz,Todd; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Synthesis and Antiprotozoal Properties of Pentamidine Congeners Bearing the Benzofuran Motif." Journal of Medicinal Chemistry. Vol. 52, no. 18. (September 2009.): 5763-5767.

Sackett,Dan,L; Werbovetz,Karl,A; Morrissette,Naomi,S. "Isolating Tubulin from Nonneural Sources." Methods in Cell Biology. Vol. 95, (January 2010.): 17-32.

Gershkovich,Pavel; Wasan,Ellen,K; Sivak,Olena; Li,Raymond; Zhu,Xiaohua; Werbovetz,Karl,A; Tidwell,Richard,R; Clement,John,G; Thornton,Sheila,J; Wasan,Kishor,M. "Visceral Leishmaniasis Affects Liver and Spleen Concentrations of Amphotericin B Following Administration to Mice." Journal of Antimicrobial Chemotherapy. Vol. 65, no. 3. (March 2010.): 535-537.

Lyons-Abbott,Sally; Sackett,Dan,L; Wloga,Dorota; Gaertig,Jacek; Morgan,Rachel,E; Werbovetz,Karl,A; Morrissette,Naomi,S. "alpha-Tubulin Mutations Alter Oryzalin Affinity and Microtubule Assembly Properties To Confer Dinitroaniline Resistance." Eukaryotic Cell. Vol. 9, no. 12. (December 2010.): 1825-1834.

Richard,Julian,V; Werbovetz,Karl,A. "New Antileishmanial Candidates and Lead Compounds." Current Opinion in Chemical Biology. Vol. 14, no. 4. (August 2010.): 447-455.

Endeshaw,Molla,M; Li,Catherine; de Leon,Jessica; Yao,Ni; Latibeaudiere,Kirk; Premalatha,Kokku; Morrissette,Naomi; Werbovetz,Karl,A. "Synthesis and Evaluation of Oryzalin Analogs against Toxoplasma gondii." Bioorganic and Medicinal Chemistry Letters. Vol. 20, no. 17. (September 2010.): 5179-5183.

Wasan,Ellen,K; Gershkovich,Pavel; Zhao,Jinying; Zhu,Xiaohua; Werbovetz,Karl; Tidwell,Richard,R; Clement,John,G; Thornton,Sheila,J; Wasan,Kishor,M. "A Novel Tropically Stable Oral Amphotericin B Formulation (iCo-010) Exhibits Efficacy against Visceral Leishmaniasis in a Murine Model." PLoS Neglected Tropical Diseases. Vol. 4, no. 12. (December 2010.): e913-.

Bakunov,Stanislav,A; Bakunova,Svetlana,M; Wenzler,Tanja; Ghebru,Maedot; Werbovetz,Karl,A; Brun,Reto; Tidwell,Richard,R. "Synthesis and Antiprotozoal Activity of Cationic 1,4-Diphenyl-1H-1,2,3-triazoles." Journal of Medicinal Chemistry. Vol. 53, no. 1. (January 2010.): 254-272.

Ma,Christopher; Tran,Johnson; Gu,Frank; Ochoa,Roxanna; Li,Catherine; Sept,David; Werbovetz,Karl; Morrissette,Naomi. "Dinitroaniline Activity in Toxoplasma gondii Expressing Wild-Type or Mutant Alpha-Tubulin." Antimicrobial Agents and Chemotherapy. Vol. 54, no. 4. (April 2010.): 1453-1460.

Fotie,Jean; Kaiser,Marcel; Delfin,Dawn,A; Manley,Joshua; Reid,Carolyn,S; Paris,Jean-Marc; Wenzler,Tanja; Maes,Louis; Mahasenan,Kiran,V; Li,Chenglong; Werbovetz,Karl,A. "Antitrypanosomal Activity of 1,2-Dihydroquinolin-6-ols and Their Ester Derivatives." Journal of Medicinal Chemistry. Vol. 53, no. 3. (February 2010.): 966-982.

Wang,Michael,Zhuo; Zhu,Xiaohua; Srivastava,Anuradha; Liu,Qiang; Sweat,J,Mark; Pandharkar,Trupti; Stephens,Chad,E; Riccio,Ed; Parman,Toufan; Munde,Manoj; Mandal,Swati; Madhubala,Rentala; Tidwell,Richard,R; Wilson,W,David; Boykin,David,W; Hall,James,Edwin; Kyle,Dennis,E; Werbovetz,Karl,A. "Novel Arylimidamides for Treatment of Visceral Leishmaniasis." Antimicrobial Agents and Chemotherapy. Vol. 54, no. 6. (June 2010.): 2507-2516.

Turabekova,Malakhat,A; Vinogradova,Valentina,I; Werbovetz,Karl,A; Capers,Jeffrey; Rasulev,Bakhtiyor,F; Levkovich,Mikhail,G; Rakhimov,Shukhrat,B; Abdullaev,Nasrulla,D. "Structure-Activity Relationship Investigations of Leishmanicidal N-Benzylcytisine Derivatives." Chemical Biology and Drug Design. Vol. 78, no. 1. (July 2011.): 183-189.

Salem,Manar,M; Capers,Jeffrey; Rito,Shawn; Werbovetz,Karl,A. "Antiparasitic Activity of C-Geranyl Flavonoids from Mimulus bigelovii." Phytotherapy Research. Vol. 25, no. 8. (August 2011.): 1246-1249.

Gershkovich,Pavel; Wasan,Kishor,M; Sivak,Olena; Lysakowski,Summer; Reid,Carolyn; Premalatha,Kokku; Werbovetz,Karl,A. "Simultaneous Determination of a Novel Antitrypanosomal Compound (OSU-36) and its Ester Derivative (OSU-40) in Plasma by HPLC: Application to First Pharmacokinetic Study in Rats." Journal of Pharmacy and Pharmaceutical Sciences. Vol. 14, no. 1. (January 2011.): 36-45.

Collar,Catharine,J; Zhu,Xiaohua; Werbovetz,Karl; Boykin,David,W; Wilson,W,David. "Molecular Factors Governing Inhibition of Arylimidamides against Leishmania: Conservative Computational Modeling to Improve Chemotherapies." Bioorganic and Medicinal Chemistry. Vol. 19, no. 15. (August 2011.): 4552-4561.

Reid,Carolyn,S; Patrick,Donald,A; He,Shanshan; Fotie,Jean; Premalatha,Kokku; Tidwell,Richard,R; Wang,Michael,Zhuo; Liu,Qiang; Gershkovich,Pavel; Wasan,Kishor,M; Wenzler,Tanja; Brun,Reto; Werbovetz,Karl,A. "Synthesis and Antitrypanosomal Evaluation of Derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of Core Substitutions and Salt Formation." Bioorganic and Medicinal Chemistry. Vol. 19, no. 1. (January 2011.): 513-523.

Bahar,Mark; Deng,Ye; Zhu,Xiaohua; He,Shanshan; Pandharkar,Trupti; Drew,Mark,E; Navarro-Vazquez,Armando; Anklin,Clemens; Gil,Roberto,R; Doskotch,Raymond,W; Werbovetz,Karl,A; Kinghorn,A,Douglas. "Potent antiprotozoal activity of a novel semi-synthetic berberine derivative." Bioorganic and Medicinal Chemistry Letters. Vol. 21, no. 9. (May 2011.): 2606-2610.

Zhu,Xiaohua; Liu,Qiang; Yang,Sihyung; Parman,Toufan; Green,Carol,E; Mirsalis,Jon,C; de Nazaré Correia Soeiro,Maria; Mello de Souza,Elen; da Silva,Cristiane,França; da Gama Jaen Batista,Denise; Stephens,Chad,E; Banerjee,Moloy; Farahat,Abdelbasset,A; Munde,Manoj; Wilson,W,David; Boykin,David,W; Wang,Michael,Zhuo; Werbovetz,Karl,A. "Evaluation of Arylimidamides DB1955 and DB1960 as Candidates against Visceral Leishmaniasis and Chagas' Disease: In Vivo Efficacy, Acute Toxicity, Pharmacokinetics, and Toxicology Studies." Antimicrobial Agents and Chemotherapy. Vol. 56, no. 7. (July 2012.): 3690-3699.

Zhu,Xiaohua; Pandharkar,Trupti; Werbovetz,Karl. "Identification of New Antileishmanial Leads from Hits Obtained by High-Throughput Screening." Antimicrobial Agents and Chemotherapy. Vol. 56, no. 3. (March 2012.): 1182-1189.

He,Shanshan; Dayton,Alex; Kuppusamy,Periannan; Werbovetz,Karl,A; Drew,Mark,E. "Induction of Oxidative Stress in Trypanosoma brucei by the Antitrypanosomal Dihydroquinoline OSU-40." Antimicrobial Agents and Chemotherapy. Vol. 56, no. 5. (May 2012.): 2428-2434.

Banerjee, M, Farahat, A, Kumar, A, Wenzler, T, Brun, R, Munde, M, Wilson, W, Zhu, X, Werbovetz, K, Boykin, D.. "Synthesis, DNA Binding and Antileishmanial Activity of Low Molecular Weight Bis-arylimidamides." European Journal of Medicinal Chemistry. -.

Reid, C, Farahat, A, Zhu, X, Pandharkar, T, Boykin, D, Werbovetz, K.. "Antileishmanial Bis-arylimidamides: DB766 Analogs Modified in the Linker Region and Bis-arylimidamide Structure–activity Relationships." Bioorganic and Medicinal Chemistry Letters. -.

 

Reference Works

August 2008 Werbovetz, Karl."Book review of "Leishmania - After the Genome"" Weinheim. : 1278

Inventions and Patents

Werbovetz, K, Brun, R, Tidwell, RR, Boykin, DW, Stephens, CE, Ismail, MA, Wilson, WD. "5,5'-Bis-(4-amidinophenyl)-2,2'-bifuran Derivatives and Related Compounds as Antiprotozoal Agents and Prodrugs Thereof." filed 2006, (patent pending), and Application No. 06114189.1

Takemoto, J, Forney, JR, Healey, MC, Yang, S, Werbovetz, KA. "Controlling Protozoan Infections using Syringomycin-family Lipodepsipeptides." Issued 2001, (patent granted), and Application No. US 1999-299266

Werbovetz, K, Franzblau, SG, Tidwell, RR, Bakunova, S, Bakunov, S. "Cationic Substituted Benzofurans as Antimicrobial Agents." Issued 2005, (patent granted), and Application No. PCT/US2004/040557

Werbovetz, K, Sackett, DL, Salem, MM. "Antileishmanial Dinitroaniline Sulfonamides with Activity against Parasite Tubulin." Issued 2005, (patent granted), and Application No. 10/512,335

Tidwell, RR, Boykin, DW, Wilson, WD, Brun, R, Hu, L, Werbovetz, K, Ismail, M, Arafa, R. "Teraryl Components as Antiparasitic Agents." Issued 2011, (patent granted), and Application No. 11/698257

Werbovetz, KA, Brendle, JJ, Boykin, DW, Stephens, CE. "Reversed Amidines and Methods of Using for Treating, Preventing, or Inhibiting Leishmaniasis." Issued 2002, (patent granted), and Application No. PCT/US01/42905

Brun, R, Werbovetz, K, Tidwell, RR, Boykin, DW, Stephens, CE, Ismail, MA, Kumar, A, Wilson, WD. "2,5-Diaryl Selenophene Compounds, Aza 2,5-Diaryl Thiophene Compounds, and their Prodrugs as Antiprotozoal Agents." Issued 2009, (patent granted), and Application No. PCT/US2008/011870

 

Presentations

"The Investigation of Tubulin as an Antileishmanial Drug Target." Presented at University of Vermont Department of Chemistry Seminar Series, Burlington, VT, US|USA. (April 1999)

"Antileishmanial Drug Discovery and Tubulin as an Antileishmanial Drug Target." Presented at Discovery of Antiparasitic Activity in Natural Products, Panama City, PA|PAN. (July 2000)

"Tubulin from Leishmania: A New Target for Antiparasitic Drugs." Presented at Miami University Department of Chemistry Seminar Series, Miami, OH, US|USA. (July 2001)

"Tubulin as a Target for New Antikinetoplastid Agents." Presented at University of Toledo College of Pharmacy Seminar Series, Toledo, OH, US|USA. (February 2005)

"Tubulin as an Antikinetoplastid Drug Target." Presented at Johns Hopkins University School of Public Health Seminar Series, Baltimore, MD, US|USA. (May 2006)

"Drug Discovery Approaches against Kinetoplastid Parasites." Presented at Duquesne University College of Pharmacy Seminar Series, Pittsburgh, PA, US|USA. (November 2008)

"Reversing the Limitations of Diamidines against Leishmaniasis." Presented at University of Nebraska College of Pharmacy Seminar Series, Omaha, NE, US|USA. (March 2010)

"Discovery and Development Efforts for Visceral Leishmaniasis." Presented at Kinetoplastid Drug Strategy Meeting, Atlanta, GA, US|USA. (November 2010)

"Drug Development for Visceral Leishmaniasis and HAT – Perspectives from the Consortium for Parasitic Drug Development (CPDD)." Presented at Neglected Tropical Diseases Meeting, Bethesda, MD, US|USA. (March 2011)

"Synthetic and Semisynthetic Alkaloids with Potent Antiparasitic Activity." Presented at University of South Florida Global Health Seminar Series, Tampa, FL, US|USA. (November 2011)

"Antiparasitic Drug Discovery: Aminoacridines to Arylimidamides." Presented at Timothy Macdonald Symposium, Charlottesville, VA, US|USA. (April 2012)

"Synthetic and Semisynthetic Alkaloids with Potent Antiparasitic Activity." Presented at University of British Columbia Faculty of Pharmacy Seminar Series, Vancouver, BC, CA|CAN. (September 2012)

 

Professional Activities

2010 - present Scientific Advisory Board, DoD Anti-parasitic Drug Research Program. Department of Defense.