Structure–activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors. Issue 21 (1st November 2016)

• Record Type: Journal Article
• Authors: Tong, Ling; Yu, Wensheng; Coburn, Craig A.; Chen, Lei; Selyutin, Oleg; Zeng, Qingbei; Dwyer, Michael P.; Nair, Anilkumar G.; Shankar, Bandarpalle B.; Kim, Seong Heon; Yang, De-Yi; Rosenblum, Stuart B.; Ruck, Rebecca T.; Davies, Ian W.; Hu, Bin; Zhong, Bin; Hao, Jinglai; Ji, Tao; Zan, Shuai; Liu, Rong; Agrawal, Sony; Carr, Donna; Curry, Stephanie; McMonagle, Patricia; Bystol, Karin; Lahser, Frederick; Ingravallo, Paul; Chen, Shiying; Asante-Appiah, Ernest; Kozlowski, Joseph A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 21(2016)
• Page Start: 5354
• Page End: 5360
• Publication Date: 2016-11-01
• Subjects: HCV NS5A inhibitor -- Elbasvir -- MK-8742 -- Direct-acting antiviral agents -- HCV infection treatment -- Indole based tetracyclic core; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.08.097
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved and flattened resistance profiles.