文献类型：期刊文献

英文题名：Disodium phosphate of novel pyrazole-linked norcantharidin analogs: Design, synthesis and their anticancer evaluation

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

机构：[1]Zhejiang Univ, Sch Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, 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：5

起止页码：346

外文期刊名：LETTERS IN DRUG DESIGN & DISCOVERY

收录：SCI-EXPANDED(收录号：WOS:000259505800008)、、Scopus(收录号：2-s2.0-47249145207)、WOS

语种：英文

外文关键词：pyrazole-linked; norcantharidin analogs; cycloadddition; disodium phosphate; anticancer evaluation; solubility

外文摘要：To design and synthesize novel pyrazole-linked norcanthridin analogs and their disodium phosphates by [3+2] 1, 3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with three hydrazines. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SMMC-7721, SGC7901, ECA109, HO-8910, K562, A549 and MCF-7 producing IC50 values from 0.07 mu M to > 100 mu M. Compound 8c showed potency for the treatment of hepatoma, with IC50 value to SMMC-7721 cell line comparable to that of norcantharidin. High potency and selectivity of compound 12 to MCF-7 cell line prove that the phosphorylation of norcantharidin analogs is an effective way to increase the activity and solubility.