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《Journal of Forestry Engineering》 2018-01
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Synthesis and antitumor activity of novel quinoline derivatives of ursolic acid

JIN Xiaoyan;CHEN Hao;TAO Xubing;WANG Shifa;GU Wen;College of Chemical Engineering,Nanjing Forestry University, Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-forest Biomass, Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals;  
A series of novel quinoline derivatives of ursolic acid( 3 a-3 f,4 a-4 f) bearing hydrazide and 1,3,4-oxadiazole moieties were synthesized by using ursolic acid,a kind of pentacyclic triterpenoid compounds,as the starting material. The structures of compounds 3 a-3 f and 4 a-4 f were characterized by IR,ESI-MS,NMR and elemental analysis.The antitumor activities of compounds 3 a-3 f and 4 a-4 f against MDA-MB-231,He La and SMMC-7721 cell lines were evaluated by MTT method. The resutls showed that compounds 3 a-3 c displayed significant antiproliferative activity. The IC50 values of compounds 3 a-3 c against MDA-MB-231,He La and SMMC-7721 cell lines were 1.16-1.84 μM,0.83-1.18 μMand 17.48-19.41 μM,respectively,which were stronger than those of the positive control etoposide. According to the antitumor activity results,the antitumor structure-activity relationship of the compounds was preliminary analyzed.It was found that the incorporation of quinolinyl groups into the ursolic acid molecule and the modification of the carboxyl group into hydrazide groups and 1,3,4-oxadiazolyl groups could significantly enhance the antitumor activity of the ursolic acid,and that the activities of hydrazide derivatives were superior to the oxadiazole derivatives. The results of this study would provide substantial basis for the future structure modification of ursolic acid and the screening for derivatives with better antitumor activities.
【Fund】: 江苏省自然科学基金(BK201516);; 江苏省绿色燃料与化学品重点实验室开放基金(JSBGFC14008);; 江苏省普通高校研究生科研创新计划项目(KYL15-089)
【CateGory Index】: TQ460.1
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