Han, Fangbin; Lin, Songwen; Liu, Peng; Tao, Jing; Yi, Chongqin; Xu, Heng published the artcile< Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives>, Application of C19H34O2, the main research area is pyridopyrimidine pyridine pyrimidine preparation anticancer antitumor agent; Anti-tumor activity; Dual inhibitor; Mammalian target of rapamycin; Phosphoinositide 3-kinase.
Inhibition of phosphoinositide 3-kinase (PI3K, phosphatidylinositol 3-kinase)/AKT/mammalian target of rapamycin (mTOR) signaling pathway by PI3K/mTOR dual inhibitors provides a promising new approach to the treatment of cancers. Target of rapamycin complex 1 (mTORC1) is a protein complex composed of TOR kinase/FRAP protein and proteins such as Raptor, GGβL, PRAS40 and Deptor (this complex is not associated with CREB-regulated transcription coactivator 1). Target of rapamycin complex 2 (mTORC2) is a protein complex composed of TOR kinase/FRAP protein and proteins such as Rictor, GβL and MAPKAP1 (this complex is not associated with CREB-regulated transcription coactivator 2). In this Letter, the authors have identified structurally novel and potent PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives Their synthesis and structure-activity relationships are reported. The synthesis of the target compounds was achieved by a coupling reaction of 6-bromo-4-methylpyrido[2,3-d]pyrimidin-2-amine with boronic acid reactants and/or aryl bromides. The title compounds thus formed included N-[5-(2-amino-4-methylpyrido[2,3-d]pyrimidin-6-yl)-2-methoxy-3-pyridinyl]-2,4-difluorobenzenesulfonamide and related substances.
Bioorganic & Medicinal Chemistry Letters published new progress about Amides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses) (pyrido[2,3-d]pyrimidine derivatives). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.
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