期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 7, 页码 1820-1824出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.02.016
关键词
Inhibitors of Apoptosis Proteins; XIAP; cIAP; Smac; Structure-based drug design; Ring-closing metathesis
The design and synthesis of a series of novel tricyclic IAP inhibitors is reported. Rapid assembly of the core tricycle involved two key steps: Rh-catalyzed hydrogenation of an unsaturated bicyclic ring system and a Ru-catalyzed ring closing alkene metathesis reaction. The final Smac mimetics bind to cIAP1 and XIAP BIR3 domains and elicit the desired phenotype in cellular proliferation assays. Dimeric IAP inhibitors were found to possess nanomolar potency in a cellular proliferation assay and favourable in vitro drug-like properties. (C) 2014 Elsevier Ltd. All rights reserved.
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