| Literature DB >> 22177405 |
Jackie D Kendall1, Patrick D O'Connor, Andrew J Marshall, Raphaël Frédérick, Elaine S Marshall, Claire L Lill, Woo-Jeong Lee, Sharada Kolekar, Mindy Chao, Alisha Malik, Shuqiao Yu, Claire Chaussade, Christina Buchanan, Gordon W Rewcastle, Bruce C Baguley, Jack U Flanagan, Stephen M F Jamieson, William A Denny, Peter R Shepherd.
Abstract
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly potent example (p110α IC(50) 0.9nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model.Entities:
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Year: 2011 PMID： 22177405 DOI： 10.1016/j.bmc.2011.11.029
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641