doi: 10.1016/j.bmcl.2008.08.064.
Epub 2008 Aug 22.
Fragment-based discovery of JAK-2 inhibitors
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- PMID: 19019674
- DOI: 10.1016/j.bmcl.2008.08.064
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Fragment-based discovery of JAK-2 inhibitors
Bioorg Med Chem Lett.
.
Abstract
Fragment-based hit identification coupled with crystallographically enabled structure-based drug design was used to design potent inhibitors of JAK-2. After two iterations from fragment 1, we were able to increase potency by greater than 500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
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