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Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
Côté B, Burch JD, Asante-Appiah E, Bayly C, Bédard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschênes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagné S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y. Côté B, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070. Epub 2013 Dec 24. Bioorg Med Chem Lett. 2014. PMID: 24412110
In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor.
Lai MT, Feng M, Falgueyret JP, Tawa P, Witmer M, DiStefano D, Li Y, Burch J, Sachs N, Lu M, Cauchon E, Campeau LC, Grobler J, Yan Y, Ducharme Y, Côté B, Asante-Appiah E, Hazuda DJ, Miller MD. Lai MT, et al. Antimicrob Agents Chemother. 2014;58(3):1652-63. doi: 10.1128/AAC.02403-13. Epub 2013 Dec 30. Antimicrob Agents Chemother. 2014. PMID: 24379202 Free PMC article.
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G. Lau CK, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):1043-8. doi: 10.1016/j.bmcl.2003.11.076. Bioorg Med Chem Lett. 2004. PMID: 15013020
The development of potent non-peptidic PTP-1B inhibitors.
Dufresne C, Roy P, Wang Z, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Ramachandran C, Kennedy BP, Xu L, Gordon R, Chan CC, Leblanc Y. Dufresne C, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):1039-42. doi: 10.1016/j.bmcl.2003.11.048. Bioorg Med Chem Lett. 2004. PMID: 15013019
Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA. Yu W, et al. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27282742
Discovery of potent macrocyclic HCV NS5A inhibitors.
Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA. Yu W, et al. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17. Bioorg Med Chem Lett. 2016. PMID: 27282743
Aryl or heteroaryl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Rosenblum SB, Zhou G, Dwyer MP, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Kim SH, Zeng Q, Selyutin O, Chen L, Masse F, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Lin M, Kozlowski JA. Yu W, et al. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3414-20. doi: 10.1016/j.bmcl.2016.06.056. Epub 2016 Jun 22. Bioorg Med Chem Lett. 2016. PMID: 27394665
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA. Yu W, et al. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30. Bioorg Med Chem Lett. 2016. PMID: 27180013
Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants.
Yu W, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Coburn CA, Selyutin O, Chen L, Rokosz L, Agrawal S, Liu R, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA. Yu W, et al. J Med Chem. 2016 Nov 23;59(22):10228-10243. doi: 10.1021/acs.jmedchem.6b01234. Epub 2016 Nov 9. J Med Chem. 2016. PMID: 27792320
62 results