Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors

Authors :: Bin Hu
Ling Tong
Sony Agrawal
Craig A. Coburn
Bandarpalle B. Shankar
Michael P. Dwyer
Bin Zhong
Lei Chen
Shiying Chen
Seong Heon Kim
Stuart B. Rosenblum
Shuai Zan
Karin Bystol
Ian W. Davies
Donna Carr
Ernest Asante-Appiah
Wensheng Yu
Joseph A. Kozlowski
Rebecca T. Ruck
Patricia McMonagle
Anilkumar G. Nair
Rong Liu
Oleg Selyutin
De-Yi Yang
Paul Ingravallo
Tao Ji
Qingbei Zeng
Jinglai Hao
Stephanie Curry
Frederick C. Lahser
Source :: Bioorganicmedicinal chemistry letters. 26(21)
Publication Year :: 2016
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.

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