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

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 act...

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Detalles Bibliográficos
Autores principales: Zhai, Xin, Huang, Qiang, Jiang, Nan, Wu, Di, Zhou, Hongyu, Gong, Ping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269785/
https://www.ncbi.nlm.nih.gov/pubmed/23459301
http://dx.doi.org/10.3390/molecules18032904
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author Zhai, Xin
Huang, Qiang
Jiang, Nan
Wu, Di
Zhou, Hongyu
Gong, Ping
author_facet Zhai, Xin
Huang, Qiang
Jiang, Nan
Wu, Di
Zhou, Hongyu
Gong, Ping
author_sort Zhai, Xin
collection PubMed
description 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 IC(50) 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.
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spelling pubmed-62697852018-12-20 Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation Zhai, Xin Huang, Qiang Jiang, Nan Wu, Di Zhou, Hongyu Gong, Ping Molecules Article 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 IC(50) 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. MDPI 2013-03-04 /pmc/articles/PMC6269785/ /pubmed/23459301 http://dx.doi.org/10.3390/molecules18032904 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Zhai, Xin
Huang, Qiang
Jiang, Nan
Wu, Di
Zhou, Hongyu
Gong, Ping
Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title_full Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title_fullStr Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title_full_unstemmed Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title_short Discovery of Hybrid Dual N-Acylhydrazone and Diaryl Urea Derivatives as Potent Antitumor Agents: Design, Synthesis and Cytotoxicity Evaluation
title_sort discovery of hybrid dual n-acylhydrazone and diaryl urea derivatives as potent antitumor agents: design, synthesis and cytotoxicity evaluation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269785/
https://www.ncbi.nlm.nih.gov/pubmed/23459301
http://dx.doi.org/10.3390/molecules18032904
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