Structure-activity relationship study of a series of caspase inhibitors containing γ-amino acid moiety for treatment of cholestatic liver disease
作者: Jianfeng MouSongliang WuZhi LuoFengying GuoHaiying HeJianhua WangFusen LinFengxun GuoJianping SunLiang ShenMinggao ZengChuan WangDeming XuZhengxian GuXin TianAiming ZhangHongjiang XuLing YangXiquan ZhangJian LiShuhui Chen
作者单位: 1WuXi AppTec (Shanghai) Co. Ltd., 288 Fute Zhong Road, Shanghai 200131, China
2Chia Tai Tianqing Pharmaceutical Group Co. Ltd., Building 9, No. 699-8, Xuanwu Road, Nanjing, Jiangsu 210023, China
刊名: Bioorganic & Medicinal Chemistry Letters, 2018, Vol.28 (10), pp.1874-1878
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2018.04.002
关键词: ApoptosisCaspase inhibitorΓ-Amino acidChronic liver disease
英文摘要: Abstract(#br)A series of caspase inhibitors containing γ-amino acid moiety have been synthesized. A systemic study on their structure-activity relationship of anti-apoptotic cellular activity is presented. These efforts led to the discovery of compound 20o as a potent caspase inhibitor, which demonstrated preclinical ameliorating total bilirubin efficacy with a significantly improved pharmacokinetic profile.
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • relationship 关系
  • treatment 处理
  • activity 活度
  • liver 
  • containing 包含的
  • cholestatic 胆汁郁积的
  • moiety 一部分
  • study 学习
  • inhibitor 抑制剂
  • series