化学研究与应用
化學研究與應用
화학연구여응용
CHEMICAL RESEARCH AND APPLICATION
2015年
6期
886-890
,共5页
刘会财%胡敏华%李家明%谢迪%左建
劉會財%鬍敏華%李傢明%謝迪%左建
류회재%호민화%리가명%사적%좌건
氯硝柳胺%环氧氯丙烷%抗肿瘤
氯硝柳胺%環氧氯丙烷%抗腫瘤
록초류알%배양록병완%항종류
niclosamide%epichlorohydrin%antitumor
以氯硝柳胺为起始原料,经醚化、亲核取代反应得到目标化合物,采用MTT法考察所合成化合物对人类乳腺癌细胞(MDA-MB-231)和人类胰腺癌细胞(ASPC-1)的体外抗肿瘤活性。合成了5个氯硝柳胺衍生物,其结构均经IR、1 H-NMR、13 C-NMR和MS确证。初步的体外抗肿瘤活性结果显示目标化合物9b和9c的抗肿瘤活性强于阳性对照药,其中化合物9b的活性对所测两种肿瘤株的抑制活性均强于阳性对照药,展现出较强的应用前景。
以氯硝柳胺為起始原料,經醚化、親覈取代反應得到目標化閤物,採用MTT法攷察所閤成化閤物對人類乳腺癌細胞(MDA-MB-231)和人類胰腺癌細胞(ASPC-1)的體外抗腫瘤活性。閤成瞭5箇氯硝柳胺衍生物,其結構均經IR、1 H-NMR、13 C-NMR和MS確證。初步的體外抗腫瘤活性結果顯示目標化閤物9b和9c的抗腫瘤活性彊于暘性對照藥,其中化閤物9b的活性對所測兩種腫瘤株的抑製活性均彊于暘性對照藥,展現齣較彊的應用前景。
이록초류알위기시원료,경미화、친핵취대반응득도목표화합물,채용MTT법고찰소합성화합물대인류유선암세포(MDA-MB-231)화인류이선암세포(ASPC-1)적체외항종류활성。합성료5개록초류알연생물,기결구균경IR、1 H-NMR、13 C-NMR화MS학증。초보적체외항종류활성결과현시목표화합물9b화9c적항종류활성강우양성대조약,기중화합물9b적활성대소측량충종류주적억제활성균강우양성대조약,전현출교강적응용전경。
The target compounds were synthesized from niclosamide by etherification and nucleophilic substitution reaction. The anti-tumor activity in vitro of these compounds have been studied by MTT assay with human breast cancer cells(MDA-MB-231)and hu-man pancreatic cells(ASPC-1). Five new compounds were synthesized,and the chemical structures were characterized by IR,1H-NMR,13 C-NMR and MS. Preliminary anti-tumor activity in vitro results showed that compound 9a-9d for inhibitory activity of tumor cell lines by differences,compounds 9b and 9c had stronger cell growth inhibitory action than the positive control drug,showing strong prospect.