Design, Synthesis and Anticancer Activities of Diaryl Urea Derivatives Bearing N-Acylhydrazone Moiety

Bei Zhang; Yanfang Zhao; Xin Zhai; Lihui Wang; Jingyu Yang; Zehui Tan; Ping Gong

doi:10.1248/cpb.c12-00234

Regular Articles

Design, Synthesis and Anticancer Activities of Diaryl Urea Derivatives Bearing N-Acylhydrazone Moiety

Bei Zhang, Yanfang Zhao, Xin Zhai, Lihui Wang, Jingyu Yang, Zehui Tan, Ping Gong

Author information

Bei Zhang
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Yanfang Zhao
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Xin Zhai
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Lihui Wang
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
Jingyu Yang
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
Zehui Tan
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
Ping Gong
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University

Keywords: diaryl urea, N-acylhydrazone, anticancer activity

JOURNAL FREE ACCESS

2012 Volume 60 Issue 8 Pages 1046-1054

DOI https://doi.org/10.1248/cpb.c12-00234

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Abstract

A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their cytotoxic activities in vitro against human lung adenocarcinoma epithelial cell line (A549), human breast cancer cell line (MDA-MB-231) and human leukemia cell line (HL-60) by standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Several compounds (1a, 1f and 1h) were further evaluated against human embryonic fibroblast, lung-derived cell line (WI38). The pharmacological results indicated that some compounds exhibited promising anticancer activities. In particular, compound 1f showed the most potent cytotoxicity against the tested three cell lines with IC₅₀ values of 0.41 µM, 0.24 µM and 0.23 µM, respectively.

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