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
- 5Citations
- 18Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 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
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85021844728&origin=inward; http://dx.doi.org/10.7324/japs.2017.70631; http://www.japsonline.com/abstract.php?article_id=2317; http://www.japsonline.com/admin/php/uploads/2317_pdf.pdf; https://dx.doi.org/10.7324/japs.2017.70631; https://www.japsonline.com/abstract.php?article_id=2317
Journal of Applied Pharmaceutical Science
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