Synthesis of a Novel Series of (E,E)-4,6-bis(styryl)-2-O-Glucopyranosyl-Pyrimidines and Their Potent Multidrug Resistance (MDR) Reversal Activity
Against Cancer Cells
stilo期刊名称: Journal of Carbohydrate Chemistry
system halted
作者: Lei Gaosupa/sup, Qian Liusupa/sup, Sumei Rensupa/sup, Shengbiao
brf
achesonWansupa/sup, Tao Jiangsupa/sup, Iris L. K. Wongsupb/sup, Larry M. C.
Chowsupb/sup,Shixi Wangsupc/sup
年份: 2012年
期号: 第8期
buzzer关键词: Curcumin;Pyrimidine;Glucosylation;Anticancer;MDR modulator年终终结
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损益表格式摘要:A novel ries of methoxy or benzyloxy substituted (E,E)-4,6-bis(styryl)-2-
方面的英文
O-glucopyranosyl-pyrimidines as curcuminoid analogs were synthesized in four
steps with total yields of 21.5% to 33.9%. A549 and HL60 cells were employed for
notionalthe anticancer activity testing. The results demonstrated that 5a, 5c, and 5e have some inhibitory activity against the HL-60 cell line. Unfortunately, no compound displayed inhibitory activity against A549 except for 5c. MDR reversal activity results demonstrated that compounds 4a (RF = 12.3) and 4b (RF = 18.5) showed strong reversal activity to the P-gp-mediated LCC6MDR cells compared to verapamil (RF = 3.2) and no cytotoxicity to cancer or normal cell lines even at a high concentrations (100 M).
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