Jinbo Zhao, Huiping Zhao, Jessica A Hall, Douglas Brown, Eileen Brandes, Joseph Bazzill, Patrick T Grogan, Chitra Subramanian, George Vielhauer, Mark S Cohen, Brian S J Blagg
Hsp90 C-terminal inhibitors are advantageous for the development of new cancer chemotherapeutics due to their ability to segregate client protein degradation from induction of the prosurvival heat shock response, which is a major detriment associated with Hsp90 N-terminal inhibitors under clinical investigation. Based upon prior SAR trends, a 1,2,3-triazole side chain was placed in lieu of the aryl side chain and attached to both the coumarin and biphenyl scaffold. Antiproliferative studies against SKBr3 and MCF-7 breast cancer cell lines demonstrated these triazole-containing compounds to exhibit improved activity...
September 1, 2014: MedChemComm