Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim
oleh: 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
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2014-03-01 |
Deskripsi
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.