Synthesis and Anti-Tumor Activity of Novel Aminomethylated Derivatives of Isoliquiritigenin

Molecules

Haoran Fu¹  Yuhang Zhang²  Xiqing Wang²  Yingzhi Han²  Xiao Peng²  Thomas Efferth³  Yujie Fu² 

[1] School of Chemistry and Environment, Beihang University, Beijing 100191, China; E-Mail:;Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, China; E-Mails:;Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, 55128 Mainz, Germany; E-Mail:

关键词: aminomethylated derivatives of isoliquiritigenin;    organic synthesis;    Mannich reaction;    anti-tumor activity;   

DOI  :  10.3390/molecules191117715

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.