Synthesis and anti-tumor activity of novel aminomethylated derivatives of isoliquiritigenin.

Abstract

A series of new aminomethylated derivatives of isoliquiritigenin was synthesized. The structures of the compounds were confirmed by IR, MS, NMR, 13C-NMR and elemental analyses. Cytotoxic activities of these derivatives towards the human prostatic cell line PC-3, human mammary cancer cell line MCF-7 and human oophoroma cell line HO-8910 in vitro were tested. The IC50 values showed cytotoxic activities of some of these new derivatives were relatively strong. Furthermore, tumor growth inhibition in vivo of aminomethylated derivatives of isoliquiritigenin 15 was superior to that of isoliquritigenin and reached inhibition rates of 71.68%. The detailed synthesis, spectroscopic data, biological and pharmacologicalactivities of the synthesized compounds were provided.

• Authors: Haoran Fu, Yuhang Zhang, Xiqing Wang, Yingzhi Han, Xiao Peng, Thomas Efferth, Yujie Fu
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 19 Issue 11 Pg. 17715-26 (Oct 31 2014) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 25365296 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Chalcones
• isoliquiritigenin

Topics

• Animals
• Antineoplastic Agents (pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Chalcones (chemistry, pharmacology)
• Drug Screening Assays, Antitumor (methods)
• Female
• Humans
• MCF-7 Cells
• Magnetic Resonance Spectroscopy (methods)
• Mice
• Mice, Inbred BALB C
• Structure-Activity Relationship