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Page 1
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Tucker TJ, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Reid JC, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y. Tucker TJ, et al. Among authors: felock pj. J Med Chem. 2008 Oct 23;51(20):6503-11. doi: 10.1021/jm800856c. Epub 2008 Oct 1. J Med Chem. 2008. PMID: 18826204
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP Jr, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJ Jr, Michelson SR, Young SD. Zhuang L, et al. Among authors: felock pj. J Med Chem. 2003 Feb 13;46(4):453-6. doi: 10.1021/jm025553u. J Med Chem. 2003. PMID: 12570367
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Guare JP, Wai JS, Gomez RP, Anthony NJ, Jolly SM, Cortes AR, Vacca JP, Felock PJ, Stillmock KA, Schleif WA, Moyer G, Gabryelski LJ, Jin L, Chen IW, Hazuda DJ, Young SD. Guare JP, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2900-4. doi: 10.1016/j.bmcl.2006.03.003. Epub 2006 Mar 22. Bioorg Med Chem Lett. 2006. PMID: 16554152
A potent and orally active HIV-1 integrase inhibitor.
Egbertson MS, Moritz HM, Melamed JY, Han W, Perlow DS, Kuo MS, Embrey M, Vacca JP, Zrada MM, Cortes AR, Wallace A, Leonard Y, Hazuda DJ, Miller MD, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Gabryelski LJ, Moyer G, Ellis JD, Jin L, Xu W, Braun MP, Kassahun K, Tsou NN, Young SD. Egbertson MS, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1392-8. doi: 10.1016/j.bmcl.2006.11.080. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17194584
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Tucker TJ, Saggar S, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y. Tucker TJ, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2008 May 1;18(9):2959-66. doi: 10.1016/j.bmcl.2008.03.064. Epub 2008 Mar 25. Bioorg Med Chem Lett. 2008. PMID: 18396399
Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.
Su DS, Lim JJ, Tinney E, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, Distefano DJ, Flynn JA, Liang Y, Sanchez R, Prasad S, Yan Y, Perlow-Poehnelt R, Torrent M, Miller M, Vacca JP, Williams TM, Anthony NJ. Su DS, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5119-23. doi: 10.1016/j.bmcl.2009.07.031. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19631528
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.
Su DS, Lim JJ, Tinney E, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, DiStefano DJ, Flynn JA, Liang Y, Sanchez R, Perlow-Poehnelt R, Miller M, Vacca JP, Williams TM, Anthony NJ. Su DS, et al. Among authors: felock pj. J Med Chem. 2009 Nov 26;52(22):7163-9. doi: 10.1021/jm901230r. J Med Chem. 2009. PMID: 19883100
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
Su DS, Lim JJ, Tinney E, Tucker TJ, Saggar S, Sisko JT, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, Distefano DJ, Flynn JA, Liang Y, Sanchez R, Perlow-Poehnelt R, Miller M, Vacca JP, Williams TM, Anthony NJ. Su DS, et al. Among authors: felock pj. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4328-32. doi: 10.1016/j.bmcl.2010.06.083. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20609585
Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors.
Lai MT, Lu M, Felock PJ, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Tynebor RM, Tucker TJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD. Lai MT, et al. Among authors: felock pj. Antimicrob Agents Chemother. 2010 Nov;54(11):4812-24. doi: 10.1128/AAC.00829-10. Epub 2010 Aug 30. Antimicrob Agents Chemother. 2010. PMID: 20805392 Free PMC article.
Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor.
Lu M, Felock PJ, Munshi V, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Gomez R, Anthony NJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD, Lai MT. Lu M, et al. Among authors: felock pj. Antimicrob Agents Chemother. 2012 Jun;56(6):3324-35. doi: 10.1128/AAC.00102-12. Epub 2012 Mar 5. Antimicrob Agents Chemother. 2012. PMID: 22391531 Free PMC article.
53 results