Document Report Card

ID: ALA1144881

Journal: J Med Chem

Title: 3,6-dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation.

Authors: Bombrun A, Gerber P, Casi G, Terradillos O, Antonsson B, Halazy S.

Abstract: There is compelling evidence that Bax channel activity stimulates cytochrome c release leading ultimately to cell death, which is a key event in ischemic injuries and neurodegenerative diseases. Here 3,6-dibromocarbazole piperazine derivatives of 2-propanol are described as the first small and potent modulators of the cytochrome c release triggered by Bid-induced Bax activation in a mitochondrial assay. Furthermore, a mechanism of action is proposed, and fluorescent derivatives allowing the localization of such inhibitors are reported.

CiteXplore: 14521400

DOI: 10.1021/jm034107j