Qin, Donghui; Lin, Xiaojuan; Liu, Zhi; Chen, Yan; Zhang, Zhiliu; Wu, Chengde; Liu, Linlin; Pan, Yan; Laquerre, Sylvie; Emery, John; Fergusson, Jeff; Roland, Kimberly; Keenan, Rick; Oliff, Allen; Kumar, Sanjay; Cheung, Mui; Su, Dai-Shi published the artcile< Discovery of Orally Bioavailable Ligand Efficient Quinazolinediones as Potent and Selective Tankyrases Inhibitors>, Formula: C4H5N3, the main research area is quinazolinedione preparation tankyrase inhibitor structure activity pharmacokinetic profile; antitumor quinazolinedione selective tankyrase inhibitor; safety quinazolinedione.
The authors report the discovery of quinazolinediones as potent and selective tankyrase inhibitors. Elucidation of the structure-activity relationship of the lead compound I (R1 = R2 = R3 = H, R4 = NHCH2Ph), led to truncated analogs, e.g., I (R1 = H, F, Cl, OMe, Me, R2 = H, F, Me, CONH2, R3 = H, CF3, Me, Cl, R4 = OH, 4-pyridylamino, 1-methyl-4-pyrazolylamino, etc.), that have good potency in cells, pharmacokinetic (PK) properties, and excellent selectivity. Compound I (R1 = R2 = H, R3 = CF3, R4 = OH) (II) exhibited excellent potencies in cells and proliferation studies, good selectivity, in vitro activities, and an excellent PK profile. Compound II also inhibited H292 xenograft tumor growth in nude mice. The synthesis, biol., pharmacokinetic, in vivo efficacy studies, and safety profiles of compounds are presented.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Formula: C4H5N3.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem