Jackie D Kendall, Anna C Giddens, Kit Yee Tsang, Elaine S Marshall, Claire L Lill, Woo-Jeong Lee, Sharada Kolekar, Mindy Chao, Alisha Malik, Shuqiao Yu, Claire Chaussade, Christina Buchanan, Stephen M F Jamieson, Gordon W Rewcastle, Bruce C Baguley, William A Denny, Peter R Shepherd
As part of our investigation into pyrazolo[1,5-a]pyridines as novel p110α selective PI3 kinase inhibitors, we report a range of analogues with improved aqueous solubility by the addition of a basic amine. The compounds demonstrated comparable p110α potency and selectivity to earlier compounds but with up to 1000× greater aqueous solubility, as the hydrochloride salts. The compounds also displayed good activity in a cellular assay of PI3 kinase activity.
November 25, 2016: Bioorganic & Medicinal Chemistry Letters