Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-x(L) 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-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.

journal_name

Mar Drugs

journal_title

Marine drugs

authors

Cheng C,Liu Y,Balasis ME,Simmons NL,Li J,Song H,Pan L,Qin Y,Nicolaou KC,Sebti SM,Li R

doi

10.3390/md12031335

subject

Has Abstract

pub_date

2014-03-07 00:00:00

pages

1335-48

issue

3

issn

1660-3397

pii

md12031335

journal_volume

12

pub_type

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