化学
多重耐药
立体化学
系列(地层学)
P-糖蛋白
生物化学
抗生素
生物
古生物学
作者
Lei Gao,Qian Liu,Sumei Ren,Shengbiao Wan,Tao Jiang,Iris L. K. Wong,Larry M.C. Chow,Shixi Wang
标识
DOI:10.1080/07328303.2012.689041
摘要
A novel series of methoxy or benzyloxy substituted (E,E)-4,6-bis(styryl)-2-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 the 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 μM).
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