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

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

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Received: 31 December 2013; in revised form: 17 February 2014 / Accepted: 18 February 2014 / Published: 7 March 2014
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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.
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

Cheng C, Liu Y, Balasis ME, Simmons NL, Li J, Song H, Pan L, Qin Y, Nicolaou KC, Sebti SM, Li R. Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim. Marine Drugs. 2014; 12(3):1335-1348.

Chicago/Turabian Style

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. 2014. "Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim." Mar. Drugs 12, no. 3: 1335-1348.


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