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N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents

OBJECTIVE(S): According to the prevalence of neoplastic diseases, there is a deep necessity for discovery of novel anticancer drugs in the field of medicinal chemistry. In the current study, a new series of phenylthiazole derivatives (compounds 4a-4f) was synthesized and their anticancer activity wa...

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Autores principales: Mohammadi-Farani, Ahmad, Foroumadi, Alireza, Kashani, Monireh Rezvani, Aliabadi, Alireza
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Mashhad University of Medical Sciences 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4242920/
https://www.ncbi.nlm.nih.gov/pubmed/25429341
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author Mohammadi-Farani, Ahmad
Foroumadi, Alireza
Kashani, Monireh Rezvani
Aliabadi, Alireza
author_facet Mohammadi-Farani, Ahmad
Foroumadi, Alireza
Kashani, Monireh Rezvani
Aliabadi, Alireza
author_sort Mohammadi-Farani, Ahmad
collection PubMed
description OBJECTIVE(S): According to the prevalence of neoplastic diseases, there is a deep necessity for discovery of novel anticancer drugs in the field of medicinal chemistry. In the current study, a new series of phenylthiazole derivatives (compounds 4a-4f) was synthesized and their anticancer activity was assessed in vitro. MATERIALS AND METHODS: All synthesized derivatives were evaluated towards three human cancerous cell lines of SKNMC (Neuroblastoma), Hep-G2 (Human hepatocarcinoma) and MCF-7 cell (Breast cancer) using MTT assay and obtained values (IC(50) ± SD) were compared with doxorubicin. RESULTS: Unfortunately, none of the synthesized compounds showed superior activity than doxorubicin against cancerous cell lines. MCF-7 cell line was the most resistant cell line against tested compounds. Compounds 4c with para nitro (IC(50) = 10.8 ± 0.08 µM) and 4d with meta chlorine (IC(50) = 11.6 ± 0.12 µM) moieties exerted the highest cytotoxic effects towards SKNMC and Hep-G2 cell lines respectively. CONCLUSION: A new series of phenylthiazole derivatives were synthesized and their anticancer activity was assessed against cancerous cell lines. More structural modifications and derivatization is necessary to achieve to the more potent compounds.
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spelling pubmed-42429202014-11-26 N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents Mohammadi-Farani, Ahmad Foroumadi, Alireza Kashani, Monireh Rezvani Aliabadi, Alireza Iran J Basic Med Sci Original Article OBJECTIVE(S): According to the prevalence of neoplastic diseases, there is a deep necessity for discovery of novel anticancer drugs in the field of medicinal chemistry. In the current study, a new series of phenylthiazole derivatives (compounds 4a-4f) was synthesized and their anticancer activity was assessed in vitro. MATERIALS AND METHODS: All synthesized derivatives were evaluated towards three human cancerous cell lines of SKNMC (Neuroblastoma), Hep-G2 (Human hepatocarcinoma) and MCF-7 cell (Breast cancer) using MTT assay and obtained values (IC(50) ± SD) were compared with doxorubicin. RESULTS: Unfortunately, none of the synthesized compounds showed superior activity than doxorubicin against cancerous cell lines. MCF-7 cell line was the most resistant cell line against tested compounds. Compounds 4c with para nitro (IC(50) = 10.8 ± 0.08 µM) and 4d with meta chlorine (IC(50) = 11.6 ± 0.12 µM) moieties exerted the highest cytotoxic effects towards SKNMC and Hep-G2 cell lines respectively. CONCLUSION: A new series of phenylthiazole derivatives were synthesized and their anticancer activity was assessed against cancerous cell lines. More structural modifications and derivatization is necessary to achieve to the more potent compounds. Mashhad University of Medical Sciences 2014-07 /pmc/articles/PMC4242920/ /pubmed/25429341 Text en © Iranian Journal of Basic Medical Sciences This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Mohammadi-Farani, Ahmad
Foroumadi, Alireza
Kashani, Monireh Rezvani
Aliabadi, Alireza
N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title_full N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title_fullStr N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title_full_unstemmed N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title_short N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Synthesis and cytotoxicity evaluation as anticancer agents
title_sort n-phenyl-2-p-tolylthiazole-4-carboxamide derivatives: synthesis and cytotoxicity evaluation as anticancer agents
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4242920/
https://www.ncbi.nlm.nih.gov/pubmed/25429341
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