Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

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

Volume 10, 8 Issues, 2014

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Medicinal Chemistry

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Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge

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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 and Jin Zhao

Affiliation: Key laboratory of Natural Medicines and Immunotechnology of Henan Province, Henan University, Kaifeng 475004, Henan, P.R. China


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
First Page: 1
Last Page: 6
Page Count: 6
DOI: 10.2174/1573406410666140428152227

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