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Molecules 2014, 19(11), 17715-17726; doi:10.3390/molecules191117715

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

1
School of Chemistry and Environment, Beihang University, Beijing 100191, China
2
Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, China
3
Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, 55128 Mainz, Germany
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 25 August 2014 / Revised: 21 October 2014 / Accepted: 27 October 2014 / Published: 31 October 2014
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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. View Full-Text
Keywords: aminomethylated derivatives of isoliquiritigenin; organic synthesis; Mannich reaction; anti-tumor activity aminomethylated derivatives of isoliquiritigenin; organic synthesis; Mannich reaction; anti-tumor activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Fu, H.; Zhang, Y.; Wang, X.; Han, Y.; Peng, X.; Efferth, T.; Fu, Y. Synthesis and Anti-Tumor Activity of Novel Aminomethylated Derivatives of Isoliquiritigenin. Molecules 2014, 19, 17715-17726.

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