1197159-95-7Relevant academic research and scientific papers
TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS
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Paragraph 0931; 0939-0940, (2017/05/19)
Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
Bis(morpholino-l,3,5-triazine) derivatives: Potent adenosine 5′-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor
Venkatesan, Aranapakam M.,Dehnhardt, Christoph M.,Delos Santos, Efren D.,Chen, Zecheng,Dos Santos, Osvald D.,Ayral-Kaloustian, Semiramis,Khafizova, Gulnaz,Brooijmans, Natasja,Mallon, Robert,Hollander, Irwin,Feldberg, Larry,Lucas, Judy,Yu, Ker,Gibbons, James,Abraham, Robert T.,Chaudhary, Inder,Mansour, Tarek S.
experimental part, p. 2636 - 2645 (2010/09/10)
The PI3K/Akt signaling pathway is a key pathway in cell proliferation, growth, survival, protein synthesis, and glucose metabolism. It has been recognized recently that inhibiting this pathway might provide a viable therapy for cancer. A series of bis(morpholino-1,3,5-triazine) derivatives were prepared and optimized to provide the highly efficacious PI3K/mTOR inhibitor 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4, 6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea 26 (PKI-587). Compound 26 has shown excellent activity in vitro and in vivo, with antitumor efficacy in both subcutaneous and orthotopic xenograft tumor models when administered intravenously. The structure-activity relationships and the in vitro and in vivo activity of analogues in this series are described.
TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS
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Page/Page column 38, (2009/12/05)
Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
