Related Experiment Video
Updated: May 15, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
3-Arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition
Huiping Zhao1, Bin Yan, Laura B Peterson
1Department of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, Kansas 66045-7563. USA.
Abstract:
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.
Related Concept Videos
Inhibition of Cdk Activity
Inhibition of CDK Activity
Drugs that Destabilize Microtubules
Abnormal Proliferation
Drugs that Stabilize Microtubules
Inhibitors of Viral Protein Synthesis

