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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