Burger, Matthew T. published the artcileSynthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors, Product Details of C4HBr3N2, the main research area is morpholino heterocyclic pyrimidine preparation phosphoinositide kinase inhibitor; PI3K/AKT pathway; phosphoinositide 3-kinase alpha.
Phosphoinositide-3-kinases (PI3K) are important oncol. targets due to the deregulation of this signaling pathway in a wide variety of human cancers. A series of 2-morpholino, 4-substituted, 6-(3-hydroxyphenyl) pyrimidines have been reported as potent inhibitors of PI3Ks. Herein, we describe the structure-guided optimization of these pyrimidines with a focus on replacing the phenol moiety, while maintaining potent target inhibition and improving in vivo properties. A series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines, which potently inhibit PI3K, were discovered. Within this series a compound (I) was identified with suitable pharmacokinetic (PK) properties, which allowed for the establishment of a PI3K PK/pharmacodynamic-efficacy relationship as determined by in vivo inhibition of AKTSer473 phosphorylation and tumor growth inhibition in a mouse A2780 tumor xenograft model.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 36847-11-7 belongs to class pyrimidines, name is 2,4,6-Tribromopyrimidine, and the molecular formula is C4HBr3N2, Product Details of C4HBr3N2.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia