Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors

A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxyphenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, i...

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Autores principales: Amirmostofian, Marzieh, Kobarfard, Farzad, Reihanfard, Hamed, Mashayekhi, Vida, Zarghi, Afshin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2015
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4277619/
https://www.ncbi.nlm.nih.gov/pubmed/25561912
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author Amirmostofian, Marzieh
Kobarfard, Farzad
Reihanfard, Hamed
Mashayekhi, Vida
Zarghi, Afshin
author_facet Amirmostofian, Marzieh
Kobarfard, Farzad
Reihanfard, Hamed
Mashayekhi, Vida
Zarghi, Afshin
author_sort Amirmostofian, Marzieh
collection PubMed
description A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxyphenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithelial cells), T47D (Human ductal breast epithelial tumor cell line) and fibroblast. According to our results, HEPG2 seems to be the most sensitive, while MCF7 was the most resistant cell line to the compounds. All the compounds expect 7b, possessed satisfactory activity against HEPG2 with mean IC(50) values ranging from 15.60 to 43.81 µM.
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spelling pubmed-42776192015-01-05 Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors Amirmostofian, Marzieh Kobarfard, Farzad Reihanfard, Hamed Mashayekhi, Vida Zarghi, Afshin Iran J Pharm Res Original Article A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxyphenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic human alveolar basal epithelial cells), T47D (Human ductal breast epithelial tumor cell line) and fibroblast. According to our results, HEPG2 seems to be the most sensitive, while MCF7 was the most resistant cell line to the compounds. All the compounds expect 7b, possessed satisfactory activity against HEPG2 with mean IC(50) values ranging from 15.60 to 43.81 µM. Shaheed Beheshti University of Medical Sciences 2015 /pmc/articles/PMC4277619/ /pubmed/25561912 Text en © 2015 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Amirmostofian, Marzieh
Kobarfard, Farzad
Reihanfard, Hamed
Mashayekhi, Vida
Zarghi, Afshin
Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title_full Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title_fullStr Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title_full_unstemmed Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title_short Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
title_sort design, synthesis and cytotoxicity evaluationof new 1,2-diaryl-4, 5, 6, 7-tetrahydro-1h-benzo[d] imidazolesas tubulin inhibitors
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4277619/
https://www.ncbi.nlm.nih.gov/pubmed/25561912
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