934545-07-0Relevant academic research and scientific papers
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.
Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors
Venkatesan, Aranapakam M.,Dehnhardt, Christoph M.,Chen, Zecheng,Santos, Efren Delos,Dos Santos, Osvaldo,Bursavich, Matthew,Gilbert, Adam M.,Ellingboe, John W.,Ayral-Kaloustian, Semiramis,Khafizova, Gulnaz,Brooijmans, Natasja,Mallon, Robert,Hollander, Irwin,Feldberg, Larry,Lucas, Judy,Yu, Ker,Gibbons, Jay,Abraham, Robert,Mansour, Tarek S.
scheme or table, p. 653 - 656 (2010/07/05)
This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3 K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of Akt at T308.
IMIDAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS PI3 KINASE AND MTOR INHIBITORS
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Page/Page column 37, (2008/12/08)
The present invention relates to Imidazolopyrimidine Analogs, methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods for treating or preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR-related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.
