Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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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.

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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: 8
Year: 2014
Page: [772 - 777]
Pages: 6
DOI: 10.2174/1573406410666140428152227
Price: $58