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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors

12 Oct 2012

Abstract excerpt

The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the pyrazolo[1,5-a]pyrimidine scaffold as a potent inhibitor of Jak2. Optimization of lead compounds 7a-b and 8 in this chemical series for activity against Jak2,...

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PMID: 23061660
DOI: 10.1021/jm3012239

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