期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 1, 页码 69-85出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.11.029
关键词
PI3 kinase; PI3K; PIK3CA; p110 alpha; Pyrazolo[1,5-a]pyridine; Sulfonohydrazide
资金
- Health Research Council of New Zealand
- Maurice Wilkins Centre for Molecular Biodiscovery
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110 alpha 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 (p110 alpha IC50 0.9 nM). 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. (C) 2011 Elsevier Ltd. All rights reserved.
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