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J Med Chem. 2008 Feb 14;51(3):373-5. doi: 10.1021/jm701385c. Epub 2008 Jan 16.

Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.

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  • 1Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA.


Heat shock protein 90 (Hsp90) is a molecular chaperone that is responsible for activating many signaling proteins and is a promising target in tumor biology. We have identified small-molecule benzisoxazole derivatives as Hsp90 inhibitors. Crystallographic studies show that these compounds bind in the ATP binding pocket interacting with the Asp93. Structure based optimization led to the identification of potent analogues, such as 13, with good biochemical profiles.

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