Synthesis and antitumor activity of licochalcone-A dihydropyrimidine derivativesChinese Full Text
Liang Cheng-yuan;Ju Wei-hui;Mao Gen-nian;Hui Nan;Sun Han;Jia Min-yi;Tian Dan-ni;Shaanxi University of Science and Technology;
Abstract: Objective To solve the problem of low water solubility of licochalcone-A and obtain its NCEs with potent antitumor activity. Methods A series of compounds of licochalcone-A dihydropyrimidine derivatives were synthesized using licochalcone-A and urea compounds as the starting materials, which have not been reported in literature before. The structure of the newly synthesized compounds were characterized by ~1H NMR, 13 C NMR and MS. Additionally, the cytotoxicity of the synthesized compounds on human prostate cancer cells（PC-3）, human lung cancer cells（A-549）, and human gastric cancer cells（SGC-7901） were further evaluated by the MTT method. Results Six licochalcone-A new derivatives were obtained, and they had significant inhibitory activity against three human cancer cell lines. Conclusion The α, β-unsaturated ketone active sites of licochalcone-A were structurally modified to improve their physicochemical properties and bioactivities, and to provide the basis for further bioactivity studies.
- DOI：
10.13461/j.cnki.cja.006003
- Series：
- Subject：
- Classification Code：
R284;R285
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