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

Sobhi M. Gomha; Nabila A. Kheder; Mohamad R. Abdelaziz; Yahia Nasser Mabkhot

doi:10.20944/preprints201608.0119.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Version 1 : Received: 10 August 2016 / Approved: 11 August 2016 / Online: 11 August 2016 (11:05:21 CEST)

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).

thiazoles; thiadiazoles; hydrazonoyl chlorides; anticancer activity; structure activity relationship

CHEMISTRY, Medicinal Chemistry

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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

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