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Int. J. Mol. Sci. 2014, 15(12), 22059-22072; doi:10.3390/ijms151222059

The Synthesis and Antiproliferative Activities of New Arylidene-Hydrazinyl-Thiazole Derivatives

1
Faculty of Pharmacy, "Iuliu Hatieganu" University of Medicine and Pharmacy, Victor Babes 41, RO-400012 Cluj-Napoca, Romania
2
Faculty of Chemistry and Chemical Engineering, University "Babes-Bolyai", M. Kogalniceanu 1, RO-400028 Cluj-Napoca, Romania
3
Research Center of Functional Genomics, Biomedicine and Translational Medicine, "Iuliu Hatieganu" University of Medicine and Pharmacy, Marinescu 23, RO-400337 Cluj-Napoca, Romania
4
Institut de Chimie, Université de Neuchâtel, Avenue de Bellevaux 51, CH-2000 Neuchâtel, Switzerland
5
Department of Immunology, "Iuliu Hatieganu" University of Medicine and Pharmacy, Victor Babes 8, RO-400012 Cluj-Napoca, Romania
*
Authors to whom correspondence should be addressed.
Received: 26 August 2014 / Revised: 12 November 2014 / Accepted: 17 November 2014 / Published: 1 December 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

New and known arylidene-hydrazinyl-thiazole derivatives have been synthesized by a convenient Hantzsch condensation. All compounds were evaluated for their in vitro cytotoxicity on two carcinoma cell lines, MDA-MB231 and HeLa. Significant antiproliferative activity for 2-(2-benzyliden-hydrazinyl)-4-methylthiazole on both MDA-MB-231 (IC50: 3.92 µg/mL) and HeLa (IC50: 11.4 µg/mL) cell lines, and for 2-[2-(4-methoxybenzylidene) hydrazinyl]-4-phenylthiazole on HeLa (IC50: 11.1 µg/mL) cell line is reported. Electrophoresis experiments showed no plasmid DNA (pTZ57R) cleavage in the presence of the investigated thiazoles. View Full-Text
Keywords: thiazole; hydrazine; cytotoxicity; DNA interaction thiazole; hydrazine; cytotoxicity; DNA interaction
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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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MDPI and ACS Style

Grozav, A.; Găină, L.I.; Pileczki, V.; Crisan, O.; Silaghi-Dumitrescu, L.; Therrien, B.; Zaharia, V.; Berindan-Neagoe, I. The Synthesis and Antiproliferative Activities of New Arylidene-Hydrazinyl-Thiazole Derivatives. Int. J. Mol. Sci. 2014, 15, 22059-22072.

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