药学研究2016，Vol.35Issue(9)：497-500,510,5.DOI:10.13506/j.cnki.jpr.2016.09.001
1-苯基-1-苯并呋喃/噻吩甲烯基环烷烃衍生物的合成及抗肿瘤活性研究
Synthesis and antitumor activity evaluation of novel 1-phenyl-1 benzofuran/benzothiopheneyl methenecycloalkane derivatives
摘要
Abstract
Objective To synthesize and evaluate antitumor activity of a series of novel 1-phenyl-1-benzofuran/benzothiopheneyl methenecycloalkane derivatives. Methods Compounds 2a ~ 2c were synthesized via condensation, Mcmurry reaction,using substituted salicylaldehydes or 2-hydroxyacetophenone( 4a~4c)as starting materials;using salicyl-aldehyde(6a)or 2-hydroxyacetophenone(6b)as starting materials,after treated with dimethylthiocarbamoyl chloride,rear-rangement,hydrolysis,condensation,Mcmurry reaction to yield 3a~3b. The antitumor activity on human CEM cells was as-sessed by MTT method.Results The structures of 5 target compounds synthesized in this paper were confirmed by 1 H-NMR,13 C-NMR and HRMS.Compounds 3a~3b showed similar antitumor activity against human leukemia cells CEM to that of lead compound 1,but all target compounds were less effective than that of Combretastatin A-4(CA-4).Conclusion Replacement the B-ring of lead compound 1 with benzothiophene resulted in the retention of antitumor activity.关键词
取代苯基-苯并呋喃/噻吩甲烯基环烷烃衍生物/血管生成抑制剂/抗肿瘤活性/合成Key words
1-phenyl-1-benzofuran/benzothiopheneylmethenecycloalkane derivatives/Vascular disrupting agents/An-titumor activity/Synthesis分类
医药卫生引用本文复制引用
刘宗英,高岩,李卓荣..1-苯基-1-苯并呋喃/噻吩甲烯基环烷烃衍生物的合成及抗肿瘤活性研究[J].药学研究,2016,35(9):497-500,510,5.基金项目
国家自然科学基金 （）
