Novel pyrazolo [1, 5-a] pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR

…, WJ Lee, S Kolekar, M Chao, A Malik, S Yu…

Index: Kendall, Jackie D.; Giddens, Anna C.; Tsang, Kit Yee; Frederick, Raphael; Marshall, Elaine S.; Singh, Ripudaman; Lill, Claire L.; Lee, Woo-Jeong; Kolekar, Sharada; Chao, Mindy; Malik, Alisha; Yu, Shuqiao; Chaussade, Claire; Buchanan, Christina; Rewcastle, Gordon W.; Baguley, Bruce C.; Flanagan, Jack U.; Jamieson, Stephen M.F.; Denny, William A.; Shepherd, Peter R. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 1 p. 58 - 68

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Citation Number: 17

Abstract

Structure–activity relationship studies of the pyrazolo [1, 5-a] pyridine class of PI3 kinase inhibitors show that substitution off the hydrazone nitrogen and replacement of the sulfonyl both gave a loss of p110α selectivity, with the exception of an N-hydroxyethyl analogue. Limited substitutions were tolerated around the phenyl ring; in particular the 2, 5-substitution pattern was important for PI3 kinase activity. The N-hydroxyethyl compound also showed ...