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FACULTY PROFILE

 
 

Edmond J. LaVoie, PhD
Professor and Chair
Department of Medicinal Chemistry

Phone: (848) 445 2674
Fax: (732) 445 6312
Email: elavoie@pharmacy.rutgers.edu

PhD, State University of New York-Buffalo

Bio

PhD, State University of New York-Buffalo

Research

Our primary research interests are in the discovery and the development of novel pharmaceuticals. For several years our research group has focused on the design and synthesis of novel non-camptothecin topoisomerase I-targeting antitumor agents. Several potent topoisomerase I-targeting agents have been identified. Studies are in progress to identify among these compounds the more promising candidates for development into the clinic. Recently, studies in our laboratory have been undertaken to develop agents that will selectively bind and stabilize G-quadruplex DNA. We are presently exploring the promise and full potential of these G-quadruplex stabilizers in cancer chemotherapy. We have also been engaged in a major research initiative to develop antibacterial agents with unique mechanisms for the treatment of severe drug-resistant infections, such as MRSA and VRE.  In addition, our group has an antiviral program focused on the development of viral endonuclease inhibitors as a new class of chemotherapeutics for the prophylaxis and treatment of influenza infection.

Representative Publications

Dorrani, M., Kaul, M., Parhi, A., LaVoie, E.J., Pilch, D.S., and Michniak-Kohn, B. (2014), TXA497 as a topical antibacterial agent: Comparative antistaphylococcal, skin deposition, and skin permeation studies with mupirocin, Int’l Journal of Pharmaceutics, 476: 199-204.

Sagong, H.Y., Bauman, J.D., Patel, D., Das, K., Arnold, E. and LaVoie, E.J. (2014), Phenyl Substituted 4-Hydroxypyridazin-3(2H)-ones and 5-Hydroxypyrimidin-4(3H)-ones: Inhibitors of Influenza A Endonuclease, Journal of Med. Chem., 57, 8086-8098.

Kaul, M., Mark, L., Zhang, Y., Parhi, A.K., LaVoie, E.J. and Pilch, D.S. (2014), Inhibiton of RND-type efflux pumps confers the FtsZ-directed prodrug TXY436 with activity against Gram-negative bacteria, Biochem. Pharmacol., 89: 321-328.

Kaul, M., Mark, L., Zhang, Y., Parhi, A.K., LaVoie, E.J. and Pilch, D.S. (2013), Pharmacokinetics and in vivo antistaphylococcal efficacy of TXY541, a 1-methylpiperidine-4-carboxamide prodrug of PC190723, Biochem. Pharmacol., 86: 1699-1707.

Bauman, J.D., Patel, D., Baker, S., Vijayan, R.S.K., Xiang, A.K., Parhi, A., Martinez-Sobrido, L., LaVoie, E.J., Das, K. and Arnold, E. (2013) Discovery of Novel Inhibitors Targeting Influenza Endonuclease by X-ray Crystallographic Fragment Screening.  ACS Chemical Biology, 8: 2501-2508.

Kaul, M., Mark, L., Zhang, Y., Parhi, A.K., LaVoie, E.J. and Pilch, D.S. (2013), TXY436: a prodrug of the FtsZ-targeting agent PC190723 with enhanced formulation properties and antistaphylococcal efficacy in vivo.  Journal of Antimicrob. Chemother., 57: 5860-5869.

Kaul, M., Zhang, Y., Parhi, A.K., LaVoie, E.J., Tusk, S., Arnold, E., Kerrigan, J.E. and Pilch, D.S. (2013) Enterococcal and streptococcal resistance to PC190723 and related compounds:  Molecular insights from a FtsZ mutational analysis.  Biochimie, 95: 1880-1887.

Parhi, A.K., Xiang, A., Bauman, J.D., Patel, D., Das, K., Vijayan, S.K., Arnold, E., and LaVoie, E.J. (2013) Phenyl substituted 3-hydroxypyridin-2(1H)-ones: Potential inhibitors of influenza A endonuclease, Bioorg. Med. Chem., 21:  6435-6446.

Blankson, G., Pilch, D.S., Liu, A., Liui, L., Rice, J.E., and LaVoie, E.J. (2013) Macrocyclic Biphenyl Tetraoxazoles: Synthesis, Evaluation as G-quadruplex Stabilizers and Cytotoxic Activity, Bioorg. Med. Chem., 21: 4511-4520.

Sagang, H.Y., Parhi, A., Bauman, J.D., Patel, D., Das, K., Vijayan, S.K., Arnold, E., and LaVoie, E.J. (2013) 3-Hydroxyquinolin(1H)-2-ones: Potential inhibitors of influenza A endonuclease, ACS Medicinal Chemistry Letters, 4: 547-550.

Blankson, G., Rzuczek, S.G., Pilch, D.S., Liu, A., Liui, L., LaVoie, E.J., and Rice, J.E. (2013) Macrocyclic Pyridyl Polyoxazoles: Structure-activity Studies of the Aminoalkyl Side-chain on G-quadruplex Stabilization and Cytotoxic Activity, Molecules, 18: 11938-11963.

Parhi, A., Zhang, Y., Saionz, K.W., Kaul, M., Pilch, D.S., and LaVoie, E.J. (2013) Antimicrobial Activity of Quinoxalines, Quinazolines, and 1,5-Naphthyridines, Bioorg. Med. Chem. Lett., 23: 4968-4974.

Zhang, Y., Giurelo, D., Parhi, A., Kaul, M. , Pilch, D.S. and LaVoie, E.J. (2013) Substituted 1,6-Diphenylnaphthalenes as Antibacterial Agents, Bioorg. Med. Chem. Lett., 23: 2001-2006.

Kelley, C., Lu, S., Parhi, A., Kaul, M., Pilch, D.S., and LaVoie, E.J. (2012) Antimicrobial Activity of Various 4- and 5-Substituted 1-Phenylnaphthalenes. Euro. J. of Med. Chem., 58, 395-409.

Kelley, C., Zhang, Y., Parhi, A., Kaul, M., Pilch, D.S., and LaVoie, E.J. (2012) 3-Phenyl Substituted 6,7-Dimethoxyisoquinoline Derivatives as FtsZ-Targeting Antibacterial Agents. Bioog. Med. Chem., 20: 7012-7029.

Kaul, M., Parhi, A.K., Zhang, Y., LaVoie, E.J., Tusk, S.,| Arnold, E., Kerrigan, J.E., and Pilch, D.S. (2012) A Bactericidal Guanidinomethyl Biaryl That Alters the Dynamics of Bacterial FtsZ Polymerization, J. Med. Chem., 55: 10160-10176.

Parhi, A., Kelley, C., ,Kaul, M., Pilch, D.S., and LaVoie, E.J. (2012) Antibacterial Activity of Substituted 5-Methylbenzo[c]phenanthridinium Derivatives Bioorg. Med. Chem. Lett., 22: 7080-7083.

Parhi, A., Lu, S., Kelley, C. , Kaul, M., Pilch, D.S. and LaVoie, E.J. (2012) Antibacterial Activity of Substituted Dibenzo[a,g]quinolizin-7-ium Derivatives. Bioorg. Med. Chem. Lett., 22: 6962-6966.