Synthesis and anti-tumor activity of 1,4-dihydrothieno[3',2':5,6] thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives  

1,4-二氢噻吩并[3',2':5,6]噻喃并[4,3-c]吡唑-3-羧酸衍生物的合成及抗癌活性研究(英文)

作　　者：孙蕊[1] 宋菁[1] 赵辉[1] 严春丽[1] 张爱君[1] Koirala Diwa 李大伟[2] 胡春[1] 

机构地区：[1]沈阳药科大学制药工程学院基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016 [2]上海交通大学药学院,上海300193

出　　处：《Journal of Chinese Pharmaceutical Sciences》2011年第1期32-36,共5页中国药学（英文版）

基　　金：National Natural Science Foundation of China (Grant No. 20474053)

摘　　要：Five 1,4-dihydrothieno[3＇,2＇：5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives were synthesized from 2- mercaptothiophene via a six-step procedure. The prepared compounds were initially evaluated for their antiprolifemtive activity using the estrogen receptors expressing MCF-7 human mammary tumor cell line in vitro. All of the prepared compounds showed moderate anti-tumor activity.本文以2-巯基噻吩为原料,经6步反应合成了5个1,4-二氢噻吩并[3',2':5,6]噻喃并[4,3-c]吡唑-3-羧酸衍生物,并采用人乳腺癌细胞MCF-7对目标化合物的抗肿瘤活性进行初步评价。所合成化合物在100μM浓度下均有一定的抑制MCF-7活性。

关 键 词：SYNTHESIS 1 4-Dihydrothieno[3＇ 2＇：5 6]thiopyrano[4 3-c]pyrazole-3-carboxylic amide derivatives Anti-tumor activity 

分 类 号：R96[医药卫生—药理学] TQ460.1[医药卫生—药学]