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Synthesis, antitumor evaluation and molecular modeling study of novel benzimidazoles and pyrazinobenzimidazoles

Journal of Applied Pharmaceutical Science, ISSN: 2231-3354, Vol: 7, Issue: 6, Page: 206-214
2017
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Article Description

Some novel benzimidazole and pyrazinobenzimidazole derivatives 5-8 was designed for evaluation of their in vitro cytotoxicity studies using MTT-based assay against three cancer cell lines namely, human hepatoma cell line (HepG2), human breast cancer cell line (MCF-7) and kidney of African green monkey (Vero B). Compounds 5a and 5c-e exhibit the highest and broad spectrum activities against all of the three cell lines tested when compared with reference drug 5-Fluorouracil (5-FU). 1-(1H-Benzimidazol-2-yl)-3-phenylprop-2-en-1-one 5a showed superior and great potency and lethal effect against HepG2, MCF-7 and Vero B cell lines with IC50 values of 2, 1.8 and 3.5μg/ml, respectively, comparable to 5-FU (IC values of 62, 12 and 13μg/ml, respectively). Moreover, compound 7b showed potent activity against MCF-7 and Vero B cell lines with IC50 values of 2 and 2.5μg/ml, respectively. Docking study of compounds 5a and 7b into the ATP binding site of epidermal growth factor receptor (EGFR) revealed comparable binding manner to an EGFR inhibitor, Erlotinib.

Bibliographic Details

Ahmed A.B. Mohamed; Azza R. Maarouf; Naglaa I. Abdel-Aziz; Alaa A.M. Abdel-Aziz; Said M. Bayomi; Farid A. Badria; Fardous ElSenduny

Journal of Applied Pharmaceutical Science

Medicine; Pharmacology, Toxicology and Pharmaceutics

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