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HCV NS5A replication complex inhibitors. Part 5: discovery of potent and pan-genotypic glycinamide cap derivatives.
Belema M, Nguyen VN, St Laurent DR, Lopez OD, Qiu Y, Good AC, Nower PT, Valera L, O'Boyle DR 2nd, Sun JH, Liu M, Fridell RA, Lemm JA, Gao M, Knipe JO, Meanwell NA, Snyder LB. Belema M, et al. Among authors: gao m. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4428-35. doi: 10.1016/j.bmcl.2013.05.040. Epub 2013 May 23. Bioorg Med Chem Lett. 2013. PMID: 23803586
Identification of hepatitis C virus NS5A inhibitors.
Lemm JA, O'Boyle D 2nd, Liu M, Nower PT, Colonno R, Deshpande MS, Snyder LB, Martin SW, St Laurent DR, Serrano-Wu MH, Romine JL, Meanwell NA, Gao M. Lemm JA, et al. Among authors: gao m. J Virol. 2010 Jan;84(1):482-91. doi: 10.1128/JVI.01360-09. J Virol. 2010. PMID: 19812153 Free PMC article.
Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.
Gao M, Nettles RE, Belema M, Snyder LB, Nguyen VN, Fridell RA, Serrano-Wu MH, Langley DR, Sun JH, O'Boyle DR 2nd, Lemm JA, Wang C, Knipe JO, Chien C, Colonno RJ, Grasela DM, Meanwell NA, Hamann LG. Gao M, et al. Nature. 2010 May 6;465(7294):96-100. doi: 10.1038/nature08960. Epub 2010 Apr 21. Nature. 2010. PMID: 20410884 Free PMC article. Clinical Trial.
Investigation of the mode of binding of a novel series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides to the hepatitis C virus polymerase.
Gentles RG, Sheriff S, Beno BR, Wan C, Kish K, Ding M, Zheng X, Chupak L, Poss MA, Witmer MR, Morin P, Wang YK, Rigat K, Lemm J, Voss S, Liu M, Pelosi L, Roberts SB, Gao M, Kadow JF. Gentles RG, et al. Among authors: gao m. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2212-5. doi: 10.1016/j.bmcl.2011.03.011. Epub 2011 Mar 6. Bioorg Med Chem Lett. 2011. PMID: 21441029
SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides: potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus.
Gentles RG, Ding M, Zheng X, Chupak L, Poss MA, Beno BR, Pelosi L, Liu M, Lemm J, Wang YK, Roberts S, Gao M, Kadow J. Gentles RG, et al. Among authors: gao m. Bioorg Med Chem Lett. 2011 May 15;21(10):3142-7. doi: 10.1016/j.bmcl.2011.03.008. Epub 2011 Mar 6. Bioorg Med Chem Lett. 2011. PMID: 21450465
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus.
Zheng X, Hudyma TW, Martin SW, Bergstrom C, Ding M, He F, Romine J, Poss MA, Kadow JF, Chang CH, Wan J, Witmer MR, Morin P, Camac DM, Sheriff S, Beno BR, Rigat KL, Wang YK, Fridell R, Lemm J, Qiu D, Liu M, Voss S, Pelosi L, Roberts SB, Gao M, Knipe J, Gentles RG. Zheng X, et al. Among authors: gao m. Bioorg Med Chem Lett. 2011 May 15;21(10):2925-9. doi: 10.1016/j.bmcl.2011.03.067. Epub 2011 Mar 23. Bioorg Med Chem Lett. 2011. PMID: 21486696
Discovery of potent hepatitis C virus NS5A inhibitors with dimeric structures.
Lemm JA, Leet JE, O'Boyle DR 2nd, Romine JL, Huang XS, Schroeder DR, Alberts J, Cantone JL, Sun JH, Nower PT, Martin SW, Serrano-Wu MH, Meanwell NA, Snyder LB, Gao M. Lemm JA, et al. Among authors: gao m. Antimicrob Agents Chemother. 2011 Aug;55(8):3795-802. doi: 10.1128/AAC.00146-11. Epub 2011 May 16. Antimicrob Agents Chemother. 2011. PMID: 21576451 Free PMC article.
Distinct functions of NS5A in hepatitis C virus RNA replication uncovered by studies with the NS5A inhibitor BMS-790052.
Fridell RA, Qiu D, Valera L, Wang C, Rose RE, Gao M. Fridell RA, et al. Among authors: gao m. J Virol. 2011 Jul;85(14):7312-20. doi: 10.1128/JVI.00253-11. Epub 2011 May 18. J Virol. 2011. PMID: 21593143 Free PMC article.
It is highly effective against genotype 1 replicons and also displays robust genotype 1 anti-HCV activity in the clinic (M. Gao et al., Nature 465:96-100, 2010). BMS-790052 inhibits genotype 2a JFH1 replicon cells and cell culture infectious virus with 50% effective …
It is highly effective against genotype 1 replicons and also displays robust genotype 1 anti-HCV activity in the clinic (M. Gao …
9,028 results