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Molecules 2016, 21(5), 579;

Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones

Dipartimento di Scienze della Vita e dell’Ambiente, Sezione di Scienze Farmaceutiche, Farmacologiche e Nutraceutiche, Università degli Studi di Cagliari, Via Ospedale 72, Cagliari I-09124, Italy
Dipartimento di Scienze della Vita e Biotecnologie, Università degli Studi di Ferrara, Via Fossato di Mortara 17-19, Ferrara I-44121, Italy
Dipartmento di Scienze Chimiche e Farmaceutiche, Università degli Studi di Ferrara, Via Fossato di Mortara 17-19, Ferrara I-44121, Italy
KU Leuven—University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven B-3000, Belgium
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 31 March 2016 / Revised: 22 April 2016 / Accepted: 25 April 2016 / Published: 30 April 2016
(This article belongs to the Section Medicinal Chemistry)
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The synthesis and antiproliferative activity of new benzimidazole derivatives bearing an hydrazone mojety at the 2-position is described. The new N′-(4-arylidene)-1H-benzo[d]imidazole-2-carbohydrazides were evaluated for their cytostatic activity toward the murine leukemia (L1210), human T-cell leukemia (CEM), human cervix carcinoma (HeLa) and human pancreas carcinoma cells (Mia Paca-2). A preliminary structure-activity relationship could be defined. Some of the compounds possess encouraging and consistent antiproliferative activity, having IC50 values in the low micromolar range. View Full-Text
Keywords: benzimidazoles; hydrazones; antiproliferative activity benzimidazoles; hydrazones; antiproliferative activity

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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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Onnis, V.; Demurtas, M.; Deplano, A.; Balboni, G.; Baldisserotto, A.; Manfredini, S.; Pacifico, S.; Liekens, S.; Balzarini, J. Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones. Molecules 2016, 21, 579.

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