Dao, Pascal; Lietha, Daniel; Etheve-Quelquejeu, Melanie; Garbay, Christiane; Chen, Huixiong published the artcile< Synthesis of novel 1,2,4-triazine scaffold as FAK inhibitors with antitumor activity>, Reference of 4956-05-2, the main research area is arylamino chlorotriazine preparation antitumor agent FAK inhibitor; structure arylamino chlorotriazine inhibition FAK antitumor activity; mol docking calculation methoxymorpholinylphenylamino methylcarbamoylphenyl chlorotriazine; 1,2,4-Triazines; Anti-cancer activity; FAK inhibitors; Molecular docking; Synthesis.
Bis(arylamino)chloro-1,2,4-triazines I [R = 3,4,5-(MeO)3C6H2, 4-H2NCH2C6H4, 4-Cl-2-MeO-5-MeC6H2, 4-(4-morpholinyl)phenyl, 2-MeO-4-(4-morpholinyl)phenyl; R1 = 3-MeSO2NHC6H4, 2-MeNHCOC6H4] were prepared as inhibitors of focal adhesion kinase (FAK) for potential use as antitumor agents; their inhibition of FAK, of human cancer cells, and of tumorigenesis in cancer cells was determined I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] inhibited FAK with an IC50 value of 230 nM and was toxic to cancer cells with IC50 values of 13 μM and 0.19 μM; colony formation in cancer cells was inhibited by I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] with IC50 values of 1.5 μM and 1.0 μM. The structure of I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] bound to FAK was determined by mol. docking calculations
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Reference of 4956-05-2.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia