文献类型：期刊文献

英文题名：Novel 1, 2, 3-triazole-linked norcantharidin analogues: Synthesis and evaluation of growth inhibition in a panel of selected tumor-cell lines

作者：Deng, Liping[1,2];Yang, Bo[1];He, Qiaojun[1];Hu, Yongzhou[1]

机构：[1]Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Sch Pharmaceut Sci, Hangzhou 310058, Peoples R China;[2]Shaoxing Univ, Dept Pharmacol, Inst Chem & Chem Engn, Shaoxing 312000, Peoples R China

年份：2008

卷号：5

期号：3

起止页码：225

外文期刊名：LETTERS IN DRUG DESIGN & DISCOVERY

收录：SCI-EXPANDED(收录号：WOS:000255864300012)、、Scopus(收录号：2-s2.0-42149191979)、WOS

语种：英文

外文关键词：1, 2, 3-triazole-linked; cantharidin; norcantharidin analogues; cycloaddition; tumor cell lines; growth inhibition

外文摘要：Twenty-one 1, 2, 3-triazole-linked norcantharidin analogues have been synthesized by the efficient [3+2]1, 3-dipolar cycloaddition reaction of norcantharidin derivatives with three organic azides. All analogues have been screened for their antiproliferative activity against a panel of tumor cell lines: KB, SMMC-7721, SGC7901, ECA109, HO8910 and K562. Compound 8e showed potency for the treatment of hepatoma, with GI(50) value (19.0 +/- 0.2 mu M) to SMMC-7721 cell line comparable to that of cantharidin (GI(50) value = 33.2 +/- 0.3 mu M).