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Volume: 9, Issue: 5, May, 2019
DOI: 10.7324/JAPS.2019.90501



Research Article

Synthesis and biological evaluation of new 2-(4-fluorophenyl) imidazol-5-ones as anticancer agents

Yasmin A. Abo-Elanwar1, Amany S. Mostafa1, Magda A. A. El-Sayed1 2, Magda N. A. Nasr1

  Author Affiliations


Abstract

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 compared 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; where varied activities were obtained. Compound 6 exhibited the highest inhibitory activity against VEGFR-2 with an IC50 value of 67 nM and moderate inhibition against CDK2A, while compound 26 achieved the best result against CDK2A with an IC50 value of 0.66 µM.

Keywords:

Imidazlone, chalcones, anticancer, VEGFR-2, CDK2A.



Citation: Abo-Elanwar YA, Mostafa AS, El-Sayed MAA, Nasr MNA. Synthesis and biological evaluation of new 2-(4-fluorophenyl) imidazol-5-ones as Anticancer Agents. J Appl Pharm Sci, 2019; 9(05):001–011.


Copyright: The Author(s). This is an open access article distributed under the Creative Commons Attribution Non-Commercial License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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