Abstract：
:A series of novel marinopyrroles with sulfide and sulphone spacers 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. Fluorescence-quenching (FQ) assays confirmed the direct binding of marinopyrroles to Mcl-1. Benzyl- and benzyl methoxy-containing sulfide derivatives 4 and 5 were highly potent dual Mcl-1/Bim and Bcl-xL/Bim disruptors (IC50 values of 600 and 700 nM), whereas carboxylate-containing sulfide derivative 9 exhibited 16.4-fold more selectivity for disrupting Mcl-1/Bim over Bcl-xL/Bim binding. In addition, a nonsymmetrical marinopyrrole 12 is as equally potent as the parent marinopyrrole A (1) for disrupting both Mcl-1/Bim and Bcl-xL/Bim binding. Some of the derivatives were also active in intact human breast cancer cells where they reduced the levels of Mcl-1, induced programd cell death (apoptosis) and inhibited cell proliferation.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Cheng C,Liu Y,Balasis ME,Garner TP,Li J,Simmons NL,Berndt N,Song H,Pan L,Qin Y,Nicolaou KC,Gavathiotis E,Sebti SM,Li Rdoi
10.3390/md12084311subject
Has Abstractpub_date
2014-07-29 00:00:00pages
4311-25issue
8issn
1660-3397pii
md12084311journal_volume
12pub_type
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