Two series of imidazolones were designed, synthesized, and evaluated for their anticancer activity against four cancer cell lines; Hela, MCF-7, PC3 and HCT-116, where four compounds 6, 25, 26 and 29 showed good potency against the whole panel. Compound 30 showed a cytotoxic effect against PC3 cell lines comparable to that of the standard doxorubicin with IC50= 8.15µM; while compounds 4 and 18 showed moderate activity with IC50 range of 10.58-11.45 µM. Enzyme inhibition assay was implemented against CDK2A and VEGFR-2 that gave varied activities. Compound 6 exhibited the highest inhibitory activity against VEGFR-2; with IC50 value of 67 nM and moderate inhibition against CDK2A, while compound 26 achieved the best result against CDK2A with IC50 value of 0.66 µM.
Key words: Imidazlone; Chalcones; Anticancer; VEGFR-2; CDK2A
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