Tetrahedron

Pyrazolyl–benzoxazole derivatives as protein kinase inhibitors. Design and validation of a combinatorial library

D Berta, M Villa, A Vulpetti, ER Felder

文献索引：Berta, Daniela; Villa, Marzia; Vulpetti, Anna; Felder, Eduard R. Tetrahedron, 2005 , vol. 61, # 45 p. 10801 - 10810

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被引用次数: 16

摘要

The malfunctioning of protein kinases is a hallmark of numerous diseases, for which a satisfactory therapy is missing. We describe the design and synthesis of a kinase targeted library based on a novel 2-(3-phenyl-1H-pyrazol-4-yl)-1, 3-benzoxazole scaffold. Ethyl 3-(3- nitrophenyl) pyrazole-4-carboxylate and its 4-nitro regioisomer were bound to trityl chloride resin, saponified with NaOH in MeOH, and amidated with a choice of two o-aminophenols. ...