Tetrahedron letters

Aryl extensions of thienopyrimidinones as fibroblast growth factor receptor 1 kinase inhibitors

AR Ekkati, V Mandiyan, KP Ravindranathan, JH Bae…

文献索引：Ekkati, Anil R.; Mandiyan, Valsan; Ravindranathan, Krishna P.; Bae, Jae H.; Schlessinger, Joseph; Jorgensen, William L. Tetrahedron Letters, 2011 , vol. 52, # 17 p. 2228 - 2231

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被引用次数: 4

摘要

Optimization of thienopyrimidinone derivatives as FGFR1 kinase inhibitors is being pursued. The present results confirm predictions of computational modeling that an aryl substituent can be introduced at the 2-position in structure 3. The substituent is anticipated to project deeper into the binding site and provide opportunities for enhanced activity and selectivity. The most potent analog reported herein, 13, has a 4-hydroxyphenyl substituent and yields ...