Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim

Chunwei Cheng; Yan Liu; Maria E. Balasis; Nicholas L. Simmons; Jerry Li; Hao Song; Lili Pan; Yong Qin; K. C. Nicolaou; Said M. Sebti; Rongshi Li

doi:10.3390/md12031335

Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim

Chunwei Cheng, Yan Liu, Maria E. Balasis, Nicholas L. Simmons, Jerry Li, Hao Song, Lili Pan, Yong Qin, K. C. Nicolaou, Said M. Sebti, Rongshi Li

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

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-X_L, 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.

Original language	English (US)
Pages (from-to)	1335-1348
Number of pages	14
Journal	Marine Drugs
Volume	12
Issue number	3
DOIs	https://doi.org/10.3390/md12031335
State	Published - Mar 2014

Keywords

Apoptosis
Cyclic marinopyrroles
Protein-protein interaction disruptors
SAR

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery
Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

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10.3390/md12031335

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title = "Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim",

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.",

keywords = "Apoptosis, Cyclic marinopyrroles, Protein-protein interaction disruptors, SAR",

author = "Chunwei Cheng and Yan Liu and Balasis, {Maria E.} and Simmons, {Nicholas L.} and Jerry Li and Hao Song and Lili Pan and Yong Qin and Nicolaou, {K. C.} and Sebti, {Said M.} and Rongshi Li",

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doi = "10.3390/md12031335",

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T1 - Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim

AU - Cheng, Chunwei

AU - Liu, Yan

AU - Balasis, Maria E.

AU - Simmons, Nicholas L.

AU - Li, Jerry

AU - Song, Hao

AU - Pan, Lili

AU - Qin, Yong

AU - Nicolaou, K. C.

AU - Sebti, Said M.

AU - Li, Rongshi

PY - 2014/3

Y1 - 2014/3

N2 - 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.

AB - 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.

KW - Apoptosis

KW - Cyclic marinopyrroles

KW - Protein-protein interaction disruptors

KW - SAR

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Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim

Abstract

Keywords

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