Cyclopeptide Smac mimetics as antagonists of IAP proteins

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Wang, Shaomeng¹ 

[1] Univ Michigan, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA

关键词: Smac mimetics;    IAP antagonists;    Apoptosis inducers;    New anticancer agents;   

DOI  :  10.1016/j.bmcl.2010.03.114

来源: Elsevier

【 摘 要 】

Two cyclopeptidic Smac mimetics, 2 and 3, were designed and synthesized. These two compounds bind to XIAP and cIAP-1/2 with low nanomolar affinities, and restore the activities of caspase-9 and caspase-3/-7 inhibited by XIAP. Compound 2 potently inhibits cancer cell growth and is 5-8 times more potent than the initial lead compound. (C) 2010 Published by Elsevier Ltd.

【 授权许可】

Free