Design,synthesis and biological evaluation of 1,4-dihydrothieno[3′,2′:5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives as potential estrogen receptor antagonists  

作　　者：Rui Sun Jing Song Si Jie Liu Hui Zhao Chun Li Yan Ai Jun Zhang Diwa Koirala Da Wei Li Chun Hu 

机构地区：[1]Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, China Department of Organic Chemistry, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China [2]School of Pharmacy, Shanghai Jiao Tong University, Shanghai 300193, China

出　　处：《Chinese Chemical Letters》2011年第3期256-259,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(NSFC)(No20474053)

摘　　要：The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women,osteoporosis, reproductive cancers such as breast cancer,uterine cancer and prostate cancer.1,4-Dihydrothieno[3＇,2＇：5,6]thiopyrano[4,3- c]pyrazole-3-carboxylic amide derivatives were designed,synthesized and biological evaluated as potential estrogen receptor antagonists.The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women,osteoporosis, reproductive cancers such as breast cancer,uterine cancer and prostate cancer.1,4-Dihydrothieno[3＇,2＇：5,6]thiopyrano[4,3- c]pyrazole-3-carboxylic amide derivatives were designed,synthesized and biological evaluated as potential estrogen receptor antagonists.

关 键 词：Estrogen receptor antagonists SYNTHESIS Biological activity Thiophene PYRAZOLE THIOPYRAN PIPERAZINE 

分 类 号：Q579.13[生物学—生物化学] TQ464.71[化学工程—制药化工]