Bioorganic and Medicinal Chemistry Letters p. 1874 - 1878 (2018)
Update date:2022-09-26
Topics:
Mou, Jianfeng
Wu, Songliang
Luo, Zhi
Guo, Fengying
He, Haiying
Wang, Jianhua
Lin, Fusen
Guo, Fengxun
Sun, Jianping
Shen, Liang
Zeng, Minggao
Wang, Chuan
Xu, Deming
Gu, Zhengxian
Tian, Xin
Zhang, Aiming
Xu, Hongjiang
Yang, Ling
Zhang, Xiquan
Li, Jian
Chen, Shuhui
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.
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