Home|Journals|Articles by Year Follow on Twitter| Subscribe to List

Directory for Medical Articles
 

Open Access

Short Communication

J App Pharm Sci. 2017; 7(6): 206-214


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

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

Abstract
ABSTRACT

A group of 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, such as 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 over HepG2, MCF-7 and Vero B cell lines with IC50 values of 2, 1.8 and 3.5g/ml, respectively, comparable to 5-FU (IC50 values of 62, 12 and 13g/ml, respectively). Moreover, compound 7b showed potent activity against MCF-7 and Vero B cell lines with IC50 values of 2 and 2.5g/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.

Key words: Prop-2-en-1-one. Benzimidazoles. Synthesis. Antitumor effect. Molecular modeling


Full-text options

Full-text Article


Share this Article


Readers of this article also read the following articles
»A choroidal malignant melanoma case with liver metastasis 15 months after diagnosis
»Azelastine hydrochloride nasal spray and its combination with fluticasone propionate in the management of allergic rhinitis - A comparative study
»A case of psychogenic movement disorder mimicking acute cerebellar syndrome
»Psychiatric Drug Prescription Patterns of Psychiatrists and Physicians of Other Specialties and Evaluation of These Treatments
»Hazard application of two common insecticides (Larvin and Sevin) on the growth, metabolic activity and nitrogen fixing capacity of cyanobacteria
»Role of antioxidants in preventing post-operative atrial fibrillation
»Arthroscopic Treatment Of Knee Degenerative Arthritis
»A case of phaeohyphomycosis causing keratitis due to Curvularia lunata
»Total and Specific Immunoglobulin E for Detection of Most Prevalent Aeroallergens in a Jordanian Cohort
»Prevalence of selected health problems among old age people at Rangampeta, Tirupati
»The effect of three fungi and their combinations on the chemical constituents of two cultivars of datepalm fruits



Advertisement
Oxidants and Antioxidants in Medical Science

SUBMIT YOUR ARTICLE NOW




ScopeMed.com
BiblioMed Home
Follow ScopeMed on Twitter
Author Tools
eJPort Journal Hosting
About BiblioMed
License Information
Terms & Conditions
Privacy Policy
Contact Us

The articles in Bibliomed are open access articles licensed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License (https://creativecommons.org/licenses/by-nc-sa/4.0/) which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
ScopeMed is a Database Service for Scientific Publications. Copyright ScopeMed Information Services.