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Mar. Drugs 2014, 12(3), 1335-1348; doi:10.3390/md12031335

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

1,5,* , 4,6
1 Key Laboratory of Drug Targeting and Drug Delivery Systems of the Ministry of Education and State Key Laboratory of Biotherapy, Department of Medicinal Natural Products, West China School of Pharmacy, Sichuan University, Chengdu 610041, China 2 Chemical Biology & Molecular Medicine Program, Department of Drug Discovery, H. Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, FL 33612, USA 3 Department of Pharmaceutical Sciences, University of Nebraska Medical Center, 985965 Nebraska Medical Center, Omaha, NE 68198, USA 4 Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA 5 The Innovative Drug Research Centre, Chongqing University, Chongqing 400000, China 6 Department of Chemistry, BioScience Research Collaborative, Rice University, 6500 Main Street, Houston, TX 77030, USA 7 Department of Oncologic Sciences, Morsani College of Medicine, University of South Florida, 12901 Bruce B. Downs, Tampa, FL 33612, USA
* Authors to whom correspondence should be addressed.
Received: 31 December 2013 / Revised: 17 February 2014 / Accepted: 18 February 2014 / Published: 7 March 2014
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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.
Keywords: cyclic marinopyrroles; protein-protein interaction disruptors; apoptosis; SAR cyclic marinopyrroles; protein-protein interaction disruptors; apoptosis; SAR
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Cheng, C.; Liu, Y.; Balasis, M.E.; Simmons, N.L.; Li, J.; Song, H.; Pan, L.; Qin, Y.; Nicolaou, K.C.; Sebti, S.M.; Li, R. Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim. Mar. Drugs 2014, 12, 1335-1348.

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