Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 8, Pages 850-855Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00226
Keywords
JAK2; selective inhibitor; myeloproliferative neoplasm; structure-guided design; BMS-911543
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JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of other diseases possessing a deregulated JAK2-STAT pathway. X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discovery of a clinical candidate, BMS-911543 (11), with excellent kinome selectivity, in vivo PD activity, and safety profile.
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