摘要
构建了不饱和硫醚类化合物对人白血病细胞K562的增殖抑制构效关系。以不饱和溴代烃和硫化物为原料,经亲核取代反应,用相转移催化剂PEG催化合成了一系列不饱和硫醚类化合物;采用MTT法(96孔板)测定系列目标产物对人白血病细胞K562的增殖抑制活性。测定结果表明:烯丙基三硫醚活性最佳,25μM抑制率达67%。
The structure-activity relationship of unsaturated thioethers related with growth inhibition on human chronic myelogenous leukemia cell K562 was explored. A library of unsaturated thioethers was prepared by parallel synthesis using the PEG catalyzed nucleophilic substitution reactions of unsaturated bromides and sulfides. The inhibition effect of these unsaturated thioethers on proliferation of K562 cell was conveniently determined upon the products directly in 96-well microtiter test plates by the commercial available MTT （tetrazolium salt） assay. This method revealed the diallyl trisulfide skeleton exhibited the highest activity： 67% of inhibition ratio under 25 μM. Structure-activity relation- ships of unsaturated thioethers related with growth inhibition on human chronic myelogenous leukemia cell K562 were constructed by comparing activities.
出处
《重庆理工大学学报（自然科学）》
CAS
2013年第5期60-64,共5页
Journal of Chongqing University of Technology：Natural Science
基金
科技部重大新药创制专项资助项目(2010ZX09401-306-2-23)
重庆理工大学研究生创新基金资助项目(YCX2011311)
