Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease PMID: 21067923

ADC Targets in Oncology

2026-04-10

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7317-22. doi: 10.1016/j.bmcl.2010.10.071.

Charles Z Ding ¹ , Yong-Kang Zhang , Xianfeng Li , Yang Liu , Suoming Zhang , Yasheen Zhou , Jacob J Plattner , Stephen J Baker , Liang Liu , Maosheng Duan , Richard L Jarvest , Jingjing Ji , Wieslaw M Kazmierski , Matthew D Tallant , Lois L Wright , Gary K Smith , Renae M Crosby , Amy A Wang , Zhi-Jie Ni , Wuxin Zou , Jon Wright

Affiliations

Abstract

We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV Protease Inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2∗ groups. P2∗ 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein.