Novel pyrazolo [1, 5-a] pyridines as PI3K inhibitors: variation of the central linker group

…, S Kolekar, M Chao, A Malik, S Yu, C Chaussade…

Index: Kendall, Jackie D.; Marshall, Andrew J.; Giddens, Anna C.; Tsang, Kit Yee; Boyd, Maruta; Frederick, Raphael; Lill, Claire L.; Lee, Woo-Jeong; Kolekar, Sharada; Chao, Mindy; Malik, Alisha; Yu, Shuqiao; Chaussade, Claire; Buchanan, Christina M.; Rewcastle, Gordon W.; Baguley, Bruce C.; Flanagan, Jack U.; Denny, William A.; Shepherd, Peter R. MedChemComm, 2014 , vol. 5, # 1 p. 41 - 46

Full Text: HTML

Citation Number: 6

Abstract

As part of our investigation into the pyrazolo [1, 5-a] pyridines as novel PI3K inhibitors, we report a range of analogues where the central linker portion of the molecule was varied while retaining the pyrazolo [1, 5-a] pyridine and arylsulfonyl or arylcarbonyl groups. Isostere generating software BROOD was used to assist with producing ideas. The isoform selectivity of the compounds varied from pan-PI3K for compound 41 to p110α-selective for ...