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

Gopalsamy, Ariamala and Shi, Mengxiao and Golas, Jennifer and Vogan, Erik and Jacob, Jaison and Johnson, Mark and Lee, Frederick and Nilakantan, Ramaswamy and Petersen, Roseann and Svenson, Kristin and Chopra, Rajiv and Tam, May S and Wen, Yingxia and Ellingboe, John and Arndt, Kim and Boschelli, Frank (2008) Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90. Journal of Medicinal Chemistry, 51 (3). pp. 373-375. ISSN 0022-2623

Abstract

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.

Item Type: Article
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Date Deposited: 14 Dec 2009 13:51
Last Modified: 31 Jan 2013 01:03
URI: https://oak.novartis.com/id/eprint/921

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