四环吲哚类NS5A抑制剂周围脯氨酸修饰的构效关系。
Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.
作者信息
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
机构信息
Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2016 Nov 1;26(21):5354-5360. doi: 10.1016/j.bmcl.2016.08.097. Epub 2016 Sep 2.
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.
我们描述了脯氨酸修饰对我们基于四环吲哚的非结构蛋白5A（NS5A）抑制剂系列的复制子图谱的影响。这项工作鉴定出了具有改善且平缓的耐药性图谱的NS5A抑制剂。
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