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Int. J. Mol. Sci. 2016, 17(9), 1499; doi:10.3390/ijms17091499

Synthesis and Characterization of Some New Bis-Pyrazolyl-Thiazoles Incorporating the Thiophene Moiety as Potent Anti-Tumor Agents

1
Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt
2
Department of Organic Chemistry, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt
3
Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia
4
Department of Measurements and Environmental Applications, National Institute of Laser Enhanced Sciences (NILES), Cairo University, Giza 12613, Egypt
*
Author to whom correspondence should be addressed.
Academic Editors: Hitoshi Sashiwa and Sanjay K. Srivastava
Received: 2 April 2016 / Revised: 24 August 2016 / Accepted: 1 September 2016 / Published: 7 September 2016
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

A new series of 1,4-bis(1-(5-(aryldiazenyl)thiazol-2-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-3-yl)benzenes 3ai were synthesized via reaction of 5,5′-(1,4-phenylene)bis(3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide) (1) with hydrazonoyl halides 2ai. In addition, reaction of 1 with ethyl chloroacetate afforded bis-thiazolone derivative 8 as the end product. Reaction of compound 8 with methyl glyoxalate gave bis-thiazolone derivative 10. The structures of the newly synthesized compounds were established on the basis of spectroscopic evidences and their alternative syntheses. All the synthesized compounds were evaluated for their anti-tumor activities against hepatocellular carcinoma (HepG2) cell lines, and the results revealed promising activities of compounds 3g, 5e, 3e, 10, 5f, 3i, and 3f with IC50 equal 1.37 ± 0.15, 1.41 ± 0.17, 1.62 ± 0.20, 1.86 ± 0.20, 1.93 ± 0.08, 2.03 ± 0.25, and 2.09 ± 0.19 μM, respectively. View Full-Text
Keywords: bis-heterocycles; bis-chalcones; hydrazonoyl halides; anticancer agents bis-heterocycles; bis-chalcones; hydrazonoyl halides; anticancer agents
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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. (CC BY 4.0).

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Gomha, S.M.; Edrees, M.M.; Altalbawy, F.M.A. Synthesis and Characterization of Some New Bis-Pyrazolyl-Thiazoles Incorporating the Thiophene Moiety as Potent Anti-Tumor Agents. Int. J. Mol. Sci. 2016, 17, 1499.

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