Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim

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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
2014
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.
Citation
Cheng, Chunwei, Liu, Yan, Balasis, Maria E., et al.. "Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim." Marine Drugs, 12, no. 3 (2014) MDPI: 1335-1348. https://doi.org/10.3390/md12031335.
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Keyword
cyclic marinopyrroles; protein-protein interaction disruptors; apoptosis; SAR
Type
Journal article
Publisher
MDPI
Citable link to this page
https://hdl.handle.net/1911/96582
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This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license
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http://creativecommons.org/licenses/by/3.0/
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This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license
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