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Page 1
Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: potent allosteric inhibitors of the hepatitis C virus NS5B polymerase.
Ding M, He F, Hudyma TW, Zheng X, Poss MA, Kadow JF, Beno BR, Rigat KL, Wang YK, Fridell RA, Lemm JA, Qiu D, Liu M, Voss S, Pelosi LA, Roberts SB, Gao M, Knipe J, Gentles RG. Ding M, et al. Among authors: lemm ja. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2866-71. doi: 10.1016/j.bmcl.2012.02.063. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22424979
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. 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
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. 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 and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Gentles RG, Ding M, Bender JA, Bergstrom CP, Grant-Young K, Hewawasam P, Hudyma T, Martin S, Nickel A, Regueiro-Ren A, Tu Y, Yang Z, Yeung KS, Zheng X, Chao S, Sun JH, Beno BR, Camac DM, Chang CH, Gao M, Morin PE, Sheriff S, Tredup J, Wan J, Witmer MR, Xie D, Hanumegowda U, Knipe J, Mosure K, Santone KS, Parker DD, Zhuo X, Lemm J, Liu M, Pelosi L, Rigat K, Voss S, Wang Y, Wang YK, Colonno RJ, Gao M, Roberts SB, Gao Q, Ng A, Meanwell NA, Kadow JF. Gentles RG, et al. Among authors: lemm j. J Med Chem. 2014 Mar 13;57(5):1855-79. doi: 10.1021/jm4016894. Epub 2014 Jan 7. J Med Chem. 2014. PMID: 24397558
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: lemm j. J Med Chem. 2017 May 25;60(10):4369-4385. doi: 10.1021/acs.jmedchem.7b00328. Epub 2017 May 4. J Med Chem. 2017. PMID: 28430437 Clinical Trial.
Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.
Parcella K, Eastman K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Liu M, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Parcella K, et al. ACS Med Chem Lett. 2017 Jun 29;8(7):771-774. doi: 10.1021/acsmedchemlett.7b00211. eCollection 2017 Jul 13. ACS Med Chem Lett. 2017. PMID: 28740615 Free PMC article.
Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.
Yeung KS, Beno BR, Mosure K, Zhu J, Grant-Young KA, Parcella K, Anjanappa P, Bora RO, Selvakumar K, Wang YK, Fang H, Krause R, Rigat K, Liu M, Lemm J, Sheriff S, Witmer M, Tredup J, Jardel A, Kish K, Parker D, Haskell R, Santone K, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Yeung KS, et al. ACS Med Chem Lett. 2018 Nov 5;9(12):1217-1222. doi: 10.1021/acsmedchemlett.8b00379. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613329 Free PMC article.
HCV NS5A replication complex inhibitors. Part 2: investigation of stilbene prolinamides.
St Laurent DR, Belema M, Gao M, Goodrich J, Kakarla R, Knipe JO, Lemm JA, Liu M, Lopez OD, Nguyen VN, Nower PT, O'Boyle D 2nd, Qiu Y, Romine JL, Serrano-Wu MH, Sun JH, Valera L, Yang F, Yang X, Meanwell NA, Snyder LB. St Laurent DR, et al. Among authors: lemm ja. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6063-6. doi: 10.1016/j.bmcl.2012.08.049. Epub 2012 Aug 21. Bioorg Med Chem Lett. 2012. PMID: 22959243
42 results