Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 11, 8 Issues, 2015


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Medicinal Chemistry

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Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents



Medicinal Chemistry, 10(8): 772-777.

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

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

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

Volume: 10
Issue Number: 8
First Page: 772
Last Page: 777
Page Count: 6
DOI: 10.2174/1573406410666140428152227
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