Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.

Basic Information

ID: ALA3414479

Journal: J Med Chem

Title: Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.

Authors: Stornaiuolo M, La Regina G, Passacantilli S, Grassia G, Coluccia A, La Pietra V, Giustiniano M, Cassese H, Di Maro S, Brancaccio D, Taliani S, Ialenti A, Silvestri R, Martini C, Novellino E, Marinelli L.

Abstract: The first direct activator of BAX, a pro-apoptotic member of the BCL-2 family, has been recently identified. Herein, a structure-based lead optimization turned out into a small series of analogues, where 8 is the most potent compound published so far. 8 was used as pharmacological tool to ascertain, for the first time, the anticancer potential of BAX direct activators and the obtained results would suggest that BAX direct activators are potential future anticancer drugs rather than venoms.

CiteXplore: 25668341

DOI: 10.1021/jm501123r

Patent ID: