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- W2048988894 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 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." @default.
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- W2048988894 date "2012-01-01" @default.
- W2048988894 modified "2023-10-11" @default.
- W2048988894 title "Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors" @default.
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- W2048988894 doi "https://doi.org/10.1016/j.bmc.2011.11.029" @default.
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