A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors |
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| Authors: | Tiansheng Wang Mark W. Ledeboer John P. Duffy Albert C. Pierce Harmon J. Zuccola Eric Block Dina Shlyakter James K. Hogan Youssef L. Bennani |
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| Affiliation: | Vertex Pharmaceuticals Inc., 130 Waverly St., Cambridge, MA 02139-4242, United States |
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| Abstract: | Pictet–Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors. |
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