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 journalArticle

10 Citations (Scopus)

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 - Jan 1 2014

Fingerprint

Apoptosis Regulatory Proteins
Enzyme-Linked Immunosorbent Assay
Proteins
marinopyrrole A

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Cheng, C., Liu, Y., Balasis, M. E., Simmons, N. L., Li, J., Song, H., ... Li, R. (2014). Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim. Marine Drugs, 12(3), 1335-1348. https://doi.org/10.3390/md12031335

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.

In: Marine Drugs, Vol. 12, No. 3, 01.01.2014, p. 1335-1348.

Research output: Contribution to journalArticle

Cheng, C, Liu, Y, Balasis, ME, Simmons, NL, Li, J, Song, H, Pan, L, Qin, Y, Nicolaou, KC, Sebti, SM & Li, R 2014, 'Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim', Marine Drugs, vol. 12, no. 3, pp. 1335-1348. https://doi.org/10.3390/md12031335
Cheng C, Liu Y, Balasis ME, Simmons NL, Li J, Song H et al. Cyclic marinopyrrole derivatives as disruptors of Mcl-1 and Bcl-xl binding to Bim. Marine Drugs. 2014 Jan 1;12(3):1335-1348. https://doi.org/10.3390/md12031335
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-xl binding to Bim. In: Marine Drugs. 2014 ; Vol. 12, No. 3. pp. 1335-1348.
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