文献类型：期刊文献

英文题名：Disodium Phosphate of Norcantharidin Analogues: Design, Synthesis and their Anticancer Evaluation

作者：Deng, Liping[1,2,3];Shen, Yongmiao[2];Wang, Wei[3];Tao, Weifeng[3];Lv, Jianguo[3];Wu, Chunlei[1]

机构：[1]Shaoxing Univ, Dept Pharm, Inst Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]Shaoxing Univ, Shaoxing Key Lab Pharm & Chem Engn, Inst Chem & Chem Engn, Shaoxing 312000, Peoples R China;[3]Zhejiang Supor Pharmaceut, Shaoxing 312000, Zhejiang, Peoples R China

年份：2009

卷号：6

期号：5

起止页码：345

外文期刊名：LETTERS IN DRUG DESIGN & DISCOVERY

收录：SCI-EXPANDED(收录号：WOS:000268218000005)、、Scopus(收录号：2-s2.0-67650566833)、WOS

基金：We thank for Zhejiang Provincial Natural Science Foundation in PRC (Y4080395).

语种：英文

外文关键词：Norcantharidin analogues; Phosphorylation; Anticancer evaluation; Solubility

外文摘要：To design and synthesize disodium phosphate of novel norcanthridin analogues. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumour cell lines: SMMC-7721, SGC7901, ECA109, A549 and MCF-7 producing IC50 values from 0.15 mu M to >50 mu M. Compounds 6 and 17 showed potency for the treatment of mammary adenocarcinoma, with IC50 value to MCF-7 cell line comparable to that of cantharidin, which proves that the phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.