1242004-38-1Relevant academic research and scientific papers
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
, p. 2904 - 2923 (2013/05/09)
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.
Design, synthesis and anticancer activities of diaryl urea derivatives bearing N-acylhydrazone moiety
Zhang, Bei,Zhao, Yanfang,Zhai, Xin,Wang, Lihui,Yang, Jingyu,Tan, Zehui,Gong, Ping
, p. 1046 - 1054 (2012/09/07)
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.
