Synthesis and biological evaluation of new 2-(4-fluorophenyl) imidazol-5-ones as anticancer agents
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Date
2019-05
Journal Title
Journal ISSN
Volume Title
Publisher
Open Science Publishers LLP
Abstract
Two series of imidazolones were designed, synthesized, and evaluated for their anticancer activity against four cancercell lines: Hela, MCF-7, PC3, and HCT-116, where four compounds 6, 25, 26, and 29 showed good potency againstthe whole panel. Compound 30 showed a cytotoxic effect against PC3 cell lines compared to that of the standarddoxorubicin with IC50 = 8.15µM, while compounds 4 and 18 showed moderate activity with IC50 range of 10.58–11.45µM. Enzyme inhibition assay was implemented against CDK2A and VEGFR-2; where varied activities were obtained.Compound 6 exhibited the highest inhibitory activity against VEGFR-2 with an IC50 value of 67 nM and moderateinhibition against CDK2A, while compound 26 achieved the best result against CDK2A with an IC50 value of 0.66 µM
Description
Keywords
Imidazlone, chalcones, anticancer, VEGFR-2, CDK2A.
Citation
Abo-Elanwar Yasmin A., Mostafa Amany S., El-Sayed Magda A. A., Nasr Magda N. A.. Synthesis and biological evaluation of new 2-(4-fluorophenyl) imidazol-5-ones as anticancer agents. Journal of Applied Pharmaceutical Science. 2019 May; 2019 May: 001-011