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.
- Cyclic marinopyrroles
- Protein-protein interaction disruptors
ASJC Scopus subject areas
- Drug Discovery