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

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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

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) 1335-1348. https://doi.org/10.3390/md12031335.

Published Version

https://doi.org/10.3390/md12031335

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

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