槲皮素O-甲基化类似物作为癌细胞增殖抑制剂的生物学评价及构效关系分析
Biological evaluation and SAR analysis of O-methylated analogs of quercetin as inhibitors of cancer cell proliferation.
作者信息
Shi Zhi-Hao, Li Nian-Guang, Tang Yu-Ping, Shi Qian-Ping, Tang Hao, Li Wei, Zhang Xu, Fu Hai-An, Duan Jin-Ao
机构信息
National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, 210023, China; Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu, 211198, China.
出版信息
Drug Dev Res. 2014 Nov;75(7):455-62. doi: 10.1002/ddr.21181. Epub 2014 Jun 27.
Using a high-throughout screening approach, the anticancer activities of 16 O-methylated (OMe) analogs of quercetin were assessed. The structure-activity relationships showed that OMe moieties at the 4' and/or 7 positions were important for maintaining inhibitory activities against the 16 cancer cell lines. Furthermore, when the OH groups at the 3' and 4' positions were both replaced by OMe moieties, anticancer activity was enhanced.
采用高通量筛选方法，评估了槲皮素的16种O-甲基化（OMe）类似物的抗癌活性。构效关系表明，4'和/或7位的OMe基团对于维持对16种癌细胞系的抑制活性很重要。此外，当3'和4'位的OH基团都被OMe基团取代时，抗癌活性增强。
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