Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

Author(s): Jianhong Wang, Huijun Zhao, Zhaoyang Luo, Zhaoyi Wang, Yahong Zhang, Jin Zhao.

Journal Name:Medicinal Chemistry

Volume 10 , Issue 8 , 2014

Graphical Abstract:


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.

Keywords: Anthrapyrazoles derivatives, cytotoxicity, topoisomerase II inhibition, polyamine.

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Article Details

Year: 2014
Page: [772 - 777]
Pages: 6
DOI: 10.2174/1573406410666140428152227
Price: $58