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Page 1
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: witmer mv. J Med Chem. 2003 Feb 13;46(4):453-6. doi: 10.1021/jm025553u. J Med Chem. 2003. PMID: 12570367
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.
Williams PD, Staas DD, Venkatraman S, Loughran HM, Ruzek RD, Booth TM, Lyle TA, Wai JS, Vacca JP, Feuston BP, Ecto LT, Flynn JA, DiStefano DJ, Hazuda DJ, Bahnck CM, Himmelberger AL, Dornadula G, Hrin RC, Stillmock KA, Witmer MV, Miller MD, Grobler JA. Williams PD, et al. Among authors: witmer mv. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6754-7. doi: 10.1016/j.bmcl.2010.08.135. Epub 2010 Sep 24. Bioorg Med Chem Lett. 2010. PMID: 20869872
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.
Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Guare JP Jr, Egbertson MS, Vacca JP, Huff JR, Felock PJ, Witmer MV, Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen IW, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PG, Schleif WA, Cortese R, Emini E, Summa V, Holloway MK, Young SD. Hazuda DJ, et al. Among authors: witmer mv. Proc Natl Acad Sci U S A. 2004 Aug 3;101(31):11233-8. doi: 10.1073/pnas.0402357101. Epub 2004 Jul 26. Proc Natl Acad Sci U S A. 2004. PMID: 15277684 Free PMC article.
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Embrey MW, Wai JS, Funk TW, Homnick CF, Perlow DS, Young SD, Vacca JP, Hazuda DJ, Felock PJ, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Wong BK, Lin JH, Leonard YM, Tsou NN, Zhuang L. Embrey MW, et al. Among authors: witmer mv. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4550-4. doi: 10.1016/j.bmcl.2005.06.105. Bioorg Med Chem Lett. 2005. PMID: 16102965
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: witmer mv. 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
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Wiscount CM, Williams PD, Tran LO, Embrey MW, Fisher TE, Sherman V, Homnick CF, Donnette Staas D, Lyle TA, Wai JS, Vacca JP, Wang Z, Felock PJ, Stillmock KA, Witmer MV, Miller MD, Hazuda DJ, Day AM, Gabryelski LJ, Ecto LT, Schleif WA, DiStefano DJ, Kochansky CJ, Anari MR. Wiscount CM, et al. Among authors: witmer mv. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4581-3. doi: 10.1016/j.bmcl.2008.07.037. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18657970
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.
Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS, Young S, Vacca J, Hazuda DJ. Grobler JA, et al. Among authors: witmer m. Proc Natl Acad Sci U S A. 2002 May 14;99(10):6661-6. doi: 10.1073/pnas.092056199. Epub 2002 May 7. Proc Natl Acad Sci U S A. 2002. PMID: 11997448 Free PMC article.
124 results