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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: embrey mw. J Med Chem. 2003 Feb 13;46(4):453-6. doi: 10.1021/jm025553u. J Med Chem. 2003. PMID: 12570367
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JP Jr, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SD. Wai JS, et al. Among authors: embrey mw. J Med Chem. 2000 Dec 28;43(26):4923-6. doi: 10.1021/jm000176b. J Med Chem. 2000. PMID: 11150161 No abstract available.
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. 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
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Wai JS, Kim B, Fisher TE, Zhuang L, Embrey MW, Williams PD, Staas DD, Culberson C, Lyle TA, Vacca JP, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Mallai R, Young SD. Wai JS, et al. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5595-9. doi: 10.1016/j.bmcl.2007.07.092. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17822898
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: embrey mw. 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
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: embrey m. 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 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: embrey m. 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
Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV.
Schreier JD, Embrey MW, Raheem IT, Barbe G, Campeau LC, Dubost D, McCabe Dunn J, Grobler J, Hartingh TJ, Hazuda DJ, Klein D, Miller MD, Moore KP, Nguyen N, Pajkovic N, Powell DA, Rada V, Sanders JM, Sisko J, Steele TG, Wai J, Walji A, Xu M, Coleman PJ. Schreier JD, et al. Among authors: embrey mw. Bioorg Med Chem Lett. 2017 May 1;27(9):2038-2046. doi: 10.1016/j.bmcl.2017.02.039. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28285916
Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.
Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ. Raheem IT, et al. Among authors: embrey m. J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26397965
153 results