Work

3-Arylcoumarin Derivatives Manifest Anti-proliferative Activity through Hsp90 Inhibition

Year: 2012

Type: article

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.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/ml300018e

Authors: Huiping Zhao, Bin Yan, Laura B. Peterson, Brian S. J. Blagg

Institution: University of Kansas

Language: English

Topic: Heat shock proteins research

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Cancer Institute