Preprint Article Version 1 NOT YET PEER-REVIEWED

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

  1. Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt
  2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Khalid University, Abha 61441, Saudi Arabia
  3. Department of pharmaceutical Chemistry, Faculty of Pharmacy, MIU University, Cairo, Egypt
  4. Department of Chemistry, College of Science, King Saud University, P. O. Box 2455, Riyadh-11451, Saudi Arabia
Version 1 : Received: 10 August 2016 / Approved: 11 August 2016 / Online: 11 August 2016 (11:05:21 CEST)

How to cite: Gomha, S.; Kheder, N.; Abdelaziz, M.; Mabkhot, Y. 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). Gomha, S.; Kheder, N.; Abdelaziz, M.; Mabkhot, Y. 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).

Subject Areas

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

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