Bioorganic and Medicinal Chemistry Letters p. 636 - 639 (2010)
Update date:2022-08-05
Topics:
Gilbert, Adam M.
Nowak, Pawel
Brooijmans, Natasja
Bursavich, Matthew G.
Dehnhardt, Christoph
Santos, Efren Delos
Feldberg, Larry R.
Hollander, Irwin
Kim, Stephen
Lombardi, Sabrina
Park, Kaapjoo
Venkatesan, Aranapakam M.
Mallon, Robert
Series of purine and pyrazolo[3,4-d]pyrimidine inhibitors of phosphatidylinositol-3-kinases (PI3K) have been prepared. The optimized purine inhibitors show good potency in a PI3K p110α (PI3K-α) fluorescence polarization assay with good selectivity versus PI3K p110γ (PI3K-γ) and the mammalian target of rapamycin (mTOR). The related pyrazolo[3,4-d]pyrimidines show potent PI3K-α and mTOR inhibition with good selectivity versus PI3K-γ. Representative compounds showed activity in a cellular proliferation assay against Caco-2 colorectal, LoVo colorectal and PC3MM2 prostate adenocarcinoma cancer cells. Signaling through the PI3K pathway was confirmed via inhibition of phospho-AKT in MDA-361 cells.
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Doi:10.1016/S0040-4039(00)84209-4
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