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5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation.


ABSTRACT: A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, 1H-NMR, and 13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.

SUBMITTER: Abu Almaaty AH 

PROVIDER: S-EPMC8003321 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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5-Aryl-1-Arylideneamino-1<i>H</i>-Imidazole-2(3<i>H</i>)-Thiones: Synthesis and In Vitro Anticancer Evaluation.

Abu Almaaty Ali H AH   Toson Eslam E M EEM   El-Sayed El-Sherbiny H EH   Tantawy Mohamed A M MAM   Fayad Eman E   Abu Ali Ola A OA   Zaki Islam I  

Molecules (Basel, Switzerland) 20210318 6


A novel series of <i>N-1</i> arylidene amino imidazole-2-thiones were synthesized, identified using IR, <sup>1</sup>H-NMR, and <sup>13</sup>C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative <b>5</b> was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles <b>4d</b> and <b>5</b> exhibit  ...[more]

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