1062204-08-3Relevant articles and documents
Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-α: Hit to lead studies
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
scheme or table, p. 636 - 639 (2010/06/14)
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.
