Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

Title:Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents

Volume: 10 Issue: 8

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

Affiliation:

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

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.

Cite this article as:

Wang Jianhong, Zhao Huijun, Luo Zhaoyang, Wang Zhaoyi, Zhang Yahong and Zhao Jin, Synthesis and Biological Activity of Anthrapyrazoles Derivatives as Potential Antitumor Agents, Medicinal Chemistry 2014; 10 (8) . https://dx.doi.org/10.2174/1573406410666140428152227