Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim
Author
Cheng, Chunwei
Liu, Yan
Balasis, Maria E.
Simmons, Nicholas L.
Li, Jerry
Song, Hao
Pan, Lili
Qin, Yong
Nicolaou, K.C.
Sebti, Said M.
Li, Rongshi
Date
2014Citation
Published Version
Abstract
A series of novel cyclic marinopyrroles were designed and synthesized. Their activity to disrupt the binding of the pro-apoptotic protein, Bim, to the pro-survival proteins, Mcl-1 and Bcl-xL, was evaluated using ELISA assays. Both atropisomers of marinopyrrole A (1) show similar potency. A tetrabromo congener 9 is two-fold more potent than 1. Two novel cyclic marinopyrroles (3 and 4) are two- to seven-fold more potent than 1.
Keyword
cyclic marinopyrroles; protein-protein interaction disruptors; apoptosis; SAR
Type
Journal article
Citable link to this page
http://hdl.handle.net/1911/96582Metadata
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