Synthesis and biological activity of anthrapyrazoles derivatives as potential antitumor agents.

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.

• Authors: Jianhong Wang, Huijun Zhao, Zhaoyang Luo, Zhaoyi Wang, Yahong Zhang, Jin Zhao
• Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 10 Issue 8 Pg. 772-7 ( 2014) ISSN: 1875-6638 [Electronic] Netherlands
• PMID: 24773347 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anthraquinones
• Antineoplastic Agents
• Polyamines
• Pyrazoles
• Mitoxantrone
• DNA Topoisomerases, Type II

Topics

• Anthraquinones (chemical synthesis, chemistry, pharmacology)
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• DNA Topoisomerases, Type II (metabolism)
• Drug Resistance, Neoplasm
• Humans
• Inhibitory Concentration 50
• Mitoxantrone (chemistry)
• Organ Specificity
• Polyamines (chemistry)
• Pyrazoles (chemical synthesis, chemistry, pharmacology)