Structure–activity relationships for 2-anilino-6-phenylpyrido [2, 3-d] pyrimidin-7 (8H)-ones as inhibitors of the cellular checkpoint kinase Wee1

…, GW Rewcastle, EM Dobrusin, A Kraker…

Index: Palmer, Brian D.; Smaill, Jeff B.; Rewcastle, Gordon W.; Dobrusin, Ellen M.; Kraker, Alan; Moore, Charles W.; Steinkampf, Randall W.; Denny, William A. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 7 p. 1931 - 1935

Full Text: HTML

Citation Number: 39

Abstract

A series of 2-anilino-6-phenylpyrido [2, 3-d] pyrimidin-7 (8H)-ones were synthesized and evaluated for their inhibitory properties against the non-receptor kinase c-Src and the G2/M checkpoint kinase Wee1. Overall, the compounds were 10–100-fold more potent inhibitors of c-Src than Wee1, and variation of substituents on the 6-phenyl ring did not markedly alter this preference. Solubilizing substituents off the 2-anilino ring in many cases increased ...