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通过 CuAAC “点击” 作为潜在的抗癌药物化学，设计、合成并制备新的抗癌活性的黄连素衍生物

 

Authors Jin X, Yan TH, Yan L, Li Q, Wang RL, Hu ZL, Jiang YY, Sun QY, Cao YB

Published Date August 2014 Volume 2014:8 Pages 1047—1059

DOI http://dx.doi.org/10.2147/DDDT.S63228

Received 27 February 2014, Accepted 23 April 2014, Published 6 August 2014

Abstract: A series of novel derivatives of phenyl-substituted berberine triazolyls has been designed and synthesized via copper-catalyzed azide-alkyne cycloaddition click chemistry in an attempt to develop antitumor agents. All of the compounds were evaluated for anticancer activity against a panel of three human cancer cell lines, including MCF-7 (breast), SW-1990 (pancreatic), and SMMC-7721 (liver) and the noncancerous human umbilical vein endothelial cell (HUVEC) cell lines. The results indicated that most of the compounds displayed notable anticancer activities against the MCF-7 cells compared with berberine. Among these derivatives, compound 16 showed the most potent inhibitory activity against the SW-1990 and SMMC-7721 cell lines, with half-maximal inhibitory concentration (IC50) values of 8.54±1.97 µM and 11.87±1.83 µM, respectively. Compound 36 exhibited the most potent inhibitory activity against the MCF-7 cell line, with an IC50 value of 12.57±1.96 µM. Compound 16 and compound 36 exhibited low cytotoxicity in the HUVEC cell line, with IC50 values of 25.49±3.24 µM and 30.47±3.47 µM. Furthermore, compounds 14, 15, 16, 17, 18, 32, and 36 exhibited much better selectivity than berberine toward the normal cell line HUVEC.
Keywords: berberine, anticancer, click chemistry, structure–activity relationship






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