期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 4, 页码 327-331出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300018e
关键词
heat shock protein 90; Hsp90 inhibitors; novobiocin; silybin; 3-arylcoumarin; breast cancer
资金
- NIH/NCI [CA120458]
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.
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