Design, Synthesis and Anticancer Activities of Diaryl Urea Derivatives Bearing N-Acylhydrazone Moiety
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概要
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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.
著者
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Zhai Xin
Key Lab Of New Drugs Design And Discovery Of Liaoning Province School Of Pharmaceutical Engineering
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Gong Ping
Key Lab Of New Drugs Design And Discovery Of Liaoning Province School Of Pharmaceutical Engineering
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Zhao Yanfang
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
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Zhao Yanfang
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Tan Zehui
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Zhang Bei
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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Wang Lihui
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
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Yang Jingyu
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
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Gong Ping
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
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