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Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

[ Vol. 10 , Issue. 8 ]


Jianhong Wang, Huijun Zhao, Zhaoyang Luo, Zhaoyi Wang, Yahong Zhang and Jin Zhao   Pages 772 - 777 ( 6 )


We have synthesized a series of anthrapyrazoles derivatives. The biological results indicated that these derivatives exhibited potent in vitro cytotoxicity against different cancer cell lines (human hepatocellular carcinoma HepG2 and BEL-7402, human colonic carcinoma HCT-116 and HT-29) and drug-resistant human hepatoma cell line (SMMC-7721). Among them, the polyamine-based anthrapyrazole derivatives 4c and 4f-g showed superior cytotoxicity than that of Mitoxantrone both on cancer cell lines and the drug-resistant subline. However, the DNA relaxation assay revealed that they had insignificant topoisomerase II inhibition. These results clearly indicate that polyamine side chains will have a profound effect on the cytotoxicity of anthrapyrazoles derivatives.


Anthrapyrazoles derivatives, cytotoxicity, topoisomerase II inhibition, polyamine.


Key Laboratory of Natural Medicines and Immunotechnology of Henan province, Henan University, kaifeng 475004, Henan, P.R. China.

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