In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 19064-73-4, name is 4-Bromophthalazin-1(2H)-one, introducing its new discovery. Recommanded Product: 4-Bromophthalazin-1(2H)-one
Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors
A series of 2,4-disubstituted phthalazinones were synthesized and their biological activities, including antiproliferation, inhibition against Aurora kinases and cell cycle effects were evaluated. Among them, N-cyclohexyl-4-((4-(1-methyl-1H-pyrazol-4-yl)-1-oxophthalazin-2(1H)-yl) methyl) benzamide (12c) exhibited the most potent antiproliferation against five carcinoma cell lines (HeLa, A549, HepG2, LoVo and HCT116 cells) with IC50 values in range of 2.2?4.6 muM, while the IC50 value of reference compound VX-680 was 8.5?15.3 muM. Moreover, Aurora kinase assays exhibited that compound 12c was potent inhibitor of AurA and AurB kinase with the IC50 values were 118 ¡À 8.1 and 80 ¡À 4.2 nM, respectively. Molecular docking studies indicated that compound 12c forms better interaction with both AurA and AurB. Furthermore, compound 12c induced G2/M cell cycle arrest in HeLa cells by regulating protein levels of cyclinB1 and cdc2. These results suggested that 12c is a promising pan-Aurora kinase inhibitor for the potential treatment of cancer.
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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N701 – PubChem