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A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety

BACKGROUND: Thiazoles and 1,3,4-thiadiazoles have been reported to possess various pharmacological activities. RESULTS: A novel series of thiazoles carrying 1,3,4-thiadiazole core were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbo-thioa...

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Autores principales: Gomha, Sobhi M., Kheder, Nabila A., Abdelaziz, Mohamad R., Mabkhot, Yahia N., Alhajoj, Ahmad M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5360743/
https://www.ncbi.nlm.nih.gov/pubmed/29086817
http://dx.doi.org/10.1186/s13065-017-0255-7
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author Gomha, Sobhi M.
Kheder, Nabila A.
Abdelaziz, Mohamad R.
Mabkhot, Yahia N.
Alhajoj, Ahmad M.
author_facet Gomha, Sobhi M.
Kheder, Nabila A.
Abdelaziz, Mohamad R.
Mabkhot, Yahia N.
Alhajoj, Ahmad M.
author_sort Gomha, Sobhi M.
collection PubMed
description BACKGROUND: Thiazoles and 1,3,4-thiadiazoles have been reported to possess various pharmacological activities. RESULTS: A novel series of thiazoles carrying 1,3,4-thiadiazole core were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbo-thioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were confirmed based on elemental and spectral analysis as well as their alternative syntheses. The cytotoxic potency of the newly synthesized thiadiazoles was evaluated by their growth inhibitory potency in liver HepG2 cancer cell line. Also, the structure activity relationship was studied. CONCLUSIONS: All the newly synthesized compounds were evaluated for their anticancer activity against liver carcinoma cell line (HepG2) using MTT assay. The results revealed that the compounds 12d, 12c, 6g, 18b, 6c, and 6f (IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) had good antitumor activity against liver carcinoma cell line (HepG2) when compared with the standard drug Doxorubicin (IC(50) = 0.72 µM). [Figure: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1186/s13065-017-0255-7) contains supplementary material, which is available to authorized users.
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spelling pubmed-53607432017-04-06 A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety Gomha, Sobhi M. Kheder, Nabila A. Abdelaziz, Mohamad R. Mabkhot, Yahia N. Alhajoj, Ahmad M. Chem Cent J Research Article BACKGROUND: Thiazoles and 1,3,4-thiadiazoles have been reported to possess various pharmacological activities. RESULTS: A novel series of thiazoles carrying 1,3,4-thiadiazole core were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbo-thioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were confirmed based on elemental and spectral analysis as well as their alternative syntheses. The cytotoxic potency of the newly synthesized thiadiazoles was evaluated by their growth inhibitory potency in liver HepG2 cancer cell line. Also, the structure activity relationship was studied. CONCLUSIONS: All the newly synthesized compounds were evaluated for their anticancer activity against liver carcinoma cell line (HepG2) using MTT assay. The results revealed that the compounds 12d, 12c, 6g, 18b, 6c, and 6f (IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) had good antitumor activity against liver carcinoma cell line (HepG2) when compared with the standard drug Doxorubicin (IC(50) = 0.72 µM). [Figure: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1186/s13065-017-0255-7) contains supplementary material, which is available to authorized users. Springer International Publishing 2017-03-21 /pmc/articles/PMC5360743/ /pubmed/29086817 http://dx.doi.org/10.1186/s13065-017-0255-7 Text en © The Author(s) 2017 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Article
Gomha, Sobhi M.
Kheder, Nabila A.
Abdelaziz, Mohamad R.
Mabkhot, Yahia N.
Alhajoj, Ahmad M.
A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title_full A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title_fullStr A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title_full_unstemmed A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title_short A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
title_sort facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5360743/
https://www.ncbi.nlm.nih.gov/pubmed/29086817
http://dx.doi.org/10.1186/s13065-017-0255-7
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