Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim

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 tetrabr...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3967213/
https://www.ncbi.nlm.nih.gov/pubmed/24608970
http://dx.doi.org/10.3390/md12031335
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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
author_facet 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
author_sort Cheng, Chunwei
collection PubMed
description 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.
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spelling pubmed-39672132014-03-27 Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim 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 Mar Drugs Article 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. MDPI 2014-03-07 /pmc/articles/PMC3967213/ /pubmed/24608970 http://dx.doi.org/10.3390/md12031335 Text en © 2014 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
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
Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title_full Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title_fullStr Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title_full_unstemmed Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title_short Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-x(L) Binding to Bim
title_sort cyclic marinopyrrole derivatives as disruptors of mcl-1 and bcl-x(l) binding to bim
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3967213/
https://www.ncbi.nlm.nih.gov/pubmed/24608970
http://dx.doi.org/10.3390/md12031335
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