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

doi:https://doi.org/10.3390/md12031335

Name:: Cyclic_Derivatives.pdf
Size:: 1.756Mb
Format:: PDF

Author

Cheng, Chunwei; Liu, Yan; Balasis, Maria E.; Simmons, Nicholas L.; Li, Jerry; More... 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.

Published Version

https://doi.org/10.3390/md12031335

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

Rights

This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license