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

doi:10.3390/molecules18032904

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

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

Xin Zhai, Qiang Huang, Nan Jiang, Di Wu, Hongyu Zhou and Ping Gong*

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China

* Author to whom correspondence should be addressed.

Received: 7 January 2013; in revised form: 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

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Cite This Article

MDPI and ACS Style

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.

AMA Style

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(3):2904-2923.

Chicago/Turabian Style

Zhai, Xin; Huang, Qiang; Jiang, Nan; Wu, Di; Zhou, Hongyu; Gong, Ping. 2013. "Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation." Molecules 18, no. 3: 2904-2923.

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