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Design,synthesis and antiproliferative activities of diaryl urea derivatives bearing N-acylhydrazone moiety
Authors:Bei Zhang a  Yan Fang Zhao a  Xin Zhai a  Wei Jie Fan a  Jun Ling Ren a  Chun Fu Wu b  Ping Gong a  a
Institution:Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China ; School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract:A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line (HL-60), human lung adenocarcinoma epithelial cell line (A549) and human breast cancer cell line (MDA-MB-231) in vitro by standard MTT assay. The pharmacological results indicated that some compounds exhibited promising antitumor activities. Compound 1j showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L, 0.7 μmol/L and 0.5 μmol/L, respectively.
Keywords:Diaryl ureas  N-Acylhydrazone  Antiproliferative activities  
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