Short Communication | Volume: 7, Issue: 6, June, 2017

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

Ahmed A. B. Mohameda,  Farid A. Badriab,  Azza R. Maaroufa,  Naglaa I. Abdel-Aziza,  Fardous ElSendunyc,  Alaa A.M. Abdel-Aziza ,  d,  Said M. Bayomia   
Ahmed A. B. Mohameda, Farid A. Badriab, Azza R. Maaroufa, Naglaa I. Abdel-Aziza, Fardous ElSendunyc, Alaa A.M. Abdel-Aziza , d, Said M. Bayomia

aDepartment of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.

bDepartment of Pharmacognosy, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.

cDepartment of Biochemistry, Faculty of Science, University of Mansoura, Mansoura, Egypt.

dDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Open Access   

Published:  Jun 30, 2017

DOI: 10.7324/JAPS.2017.70631
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Abstract

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 (IC50 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.



Citation:

Mohamed AAB, Badria FA, Maarouf AR, Abdel-Aziz NI, ElSenduny F, Abdel-Aziz AM, Bayomi SM. Synthesis, antitumor evaluation and molecular modeling study of novel benzimidazoles and pyrazinobenzimidazoles. J App Pharm Sci, 2017; 7 (06): 206- 214.

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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