Discovery and biological activity of 6BrCaQ as an inhibitor of the Hsp90 protein folding machinery

…, D Methy??Gonnot, C Radanyi, JM Renoir…

Index: Audisio, Davide; Messaoudi, Samir; Cegielkowski, Lukasz; Peyrat, Jean-Francois; Brion, Jean-Daniel; Methy-Gonnot, Delphine; Radanyi, Christine; Renoir, Jack-Michel; Alami, Mouad ChemMedChem, 2011 , vol. 6, # 5 p. 804 - 815

Full Text: HTML

Citation Number: 23

Abstract

Abstract Heat shock protein 90 (Hsp90) is a significant target in the development of rational cancer therapy, due to its role at the crossroads of multiple signaling pathways associated with cell proliferation and viability. Here, a novel series of Hsp90 inhibitors containing a quinolein-2-one scaffold was synthesized and evaluated in cell proliferation assays. Results from these structure–activity relationships studies enabled identification of the simplified 3- ...