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Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
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The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor
Jatinder Kaur1, Atul Bhardwaj1, Bruce J Melancon1
1Warren Family Research Center for Drug Discovery and Development, Department of Chemistry and Biochemistry,University of Notre Dame, Notre Dame, Indiana, USA.
Synthetic Communications
|October 23, 2020
Abstract:
AT13387 is an orally bioavailable clinical candidate developed to inhibit theheat shock protein 90 (Hsp90). This article describes a modified synthetic route for the multi-gram production of AT13387 in 46% overall yield. The modified synthetic route is short, avoids stringent reaction conditions and difficult purifications, which led to increase in an overall yield.
