Design, synthesis and biological evaluation of alkylamino biphenylamides as Hsp90 C-terminal inhibitors.

ABSTRACT: Hsp90 is a promising therapeutic target for the development of anti-cancer agents due to its integral role in the stability and function of proteins associated with all ten hallmarks of cancer. Novobiocin, a coumarin antibiotic, was the first natural product identified that targeted the Hsp90 C-terminal domain and manifested anti-proliferative activity (SKBr3 IC₅₀∼700μM). Subsequent structural investigations on novobiocin led to analogues with significantly improved anti-proliferative activity against multiple cancer cell lines. In an effort to develop more efficacious and diverse analogues, it was recently found that the coumarin ring of novobiocin could be replaced with the biphenyl core without compromising activity. Based on these prior studies, a series of alkylamino biphen

SUBMITTER: Garg G 

PROVIDER: S-EPMC5214847 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature