| Literature DB >> 27923617 |
Jackie D Kendall1, Anna C Giddens2, Kit Yee Tsang2, Elaine S Marshall2, Claire L Lill3, Woo-Jeong Lee3, Sharada Kolekar3, Mindy Chao3, Alisha Malik3, Shuqiao Yu3, Claire Chaussade4, Christina Buchanan4, Stephen M F Jamieson5, Gordon W Rewcastle5, Bruce C Baguley5, William A Denny5, Peter R Shepherd4.
Abstract
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.Entities:
Keywords: Aqueous solubility; P110α; PI3 kinase; PI3K; Pyrazolo[1,5-a]pyridine; Sulfonohydrazide
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Year: 2016 PMID： 27923617 DOI： 10.1016/j.bmcl.2016.11.078
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823