1361199-03-2Relevant academic research and scientific papers
3-arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition
Zhao, Huiping,Yan, Bin,Peterson, Laura B.,Blagg, Brian S. J.
, p. 327 - 331 (2012/05/20)
The potential therapeutic benefits associated with Hsp90 modulation for the treatment of cancer and neurodegenerative diseases highlight the importance of identifying novel Hsp90 scaffolds. KU-398, a novobiocin analogue, and silybin were recently identified as new Hsp90 inhibitors. Consequently, a library of 3-arylcoumarin derivatives that incorporated the structural features of KU-398 and silybin was designed, synthesized, and evaluated against two breast cancer cell lines. Western blot analysis confirmed that the resulting 3-arylcoumarin hybrids target the Hsp90 protein folding machinery.
