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 journalArticlepeer-review

10 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-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.

Original languageEnglish (US)
Pages (from-to)1335-1348
Number of pages14
JournalMarine Drugs
Volume12
Issue number3
DOIs
StatePublished - Mar 2014

Keywords

  • Apoptosis
  • Cyclic marinopyrroles
  • Protein-protein interaction disruptors
  • SAR

ASJC Scopus subject areas

  • Drug Discovery

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