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A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship
Version 1
: Received: 10 August 2016 / Approved: 11 August 2016 / Online: 11 August 2016 (11:05:21 CEST)
How to cite:
Gomha, S.M.; Kheder, N.A.; Abdelaziz, M.R.; Mabkhot, Y.N. A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship. Preprints2016, 2016080119 (doi: 10.20944/preprints201608.0119.v1).
Gomha, S.M.; Kheder, N.A.; Abdelaziz, M.R.; Mabkhot, Y.N. A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship. Preprints 2016, 2016080119 (doi: 10.20944/preprints201608.0119.v1).
Cite as:
Gomha, S.M.; Kheder, N.A.; Abdelaziz, M.R.; Mabkhot, Y.N. A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship. Preprints2016, 2016080119 (doi: 10.20944/preprints201608.0119.v1).
Gomha, S.M.; Kheder, N.A.; Abdelaziz, M.R.; Mabkhot, Y.N. A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship. Preprints 2016, 2016080119 (doi: 10.20944/preprints201608.0119.v1).
Abstract
A novel series of thiazole based-1,3,4-thiadiazoles were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbothioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were established based on spectroscopic evidences and their alternative syntheses. Thirteen new 1,3,4-thiadiazoles have been evaluated for their anticancer activity against liver carcinoma cell line (HepG2). Also, their structure activity relationship (SAR) was studied. The 1,3,4-thiadiazoles 12d, 12c, 6g,18b, 6c, and 6f(IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) have promising antitumor activity against liver carcinoma cell line (HepG2).
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.