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Molecules 2013, 18(3), 2904-2923; doi:10.3390/molecules18032904
Article

Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation

, , , ,  and *
Received: 7 January 2013 / Revised: 19 January 2013 / Accepted: 25 January 2013 / Published: 4 March 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Based on the hybrid pharmacophore design concept, a novel series of dual diaryl urea and N-acylhydrazone derivatives were synthesized and evaluated for their in vitro cytotoxicity by the standard MTT assay. The pharmacological results indicated that most compounds exhibited moderate to excellent activity. Moreover, compound 2g showed the most potent cytotoxicity against HL-60, A549 and MDA-MB-231 cell lines, with IC50 values of 0.22, 0.34 and 0.41 μM, respectively, which was 3.8 to 22.5 times more active than the reference compounds sorafenib and PAC-1. The promising compound 2g thus emerges as a lead for further structural modifications.
Keywords: diaryl ureas; N-acylhydrazone; cytotoxicity diaryl ureas; N-acylhydrazone; cytotoxicity
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.

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Zhai, X.; Huang, Q.; Jiang, N.; Wu, D.; Zhou, H.; Gong, P. Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation. Molecules 2013, 18, 2904-2923.

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