Citation: Rui Sun, Jing Song, Si Jie Liu, Hui Zhao, Chun Li Yan, Ai Jun Zhang, Diwa Koirala, Da Wei Li, Chun Hu. 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[J]. Chinese Chemical Letters, ;2011, 22(3): 256-259. doi: 10.1016/j.cclet.2010.10.029 shu

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

Rui Sun ^a, ,
Jing Song ^a ,
Si Jie Liu ^a ,
Hui Zhao ^a ,
Chun Li Yan ^a ,
Ai Jun Zhang ^a ,
Diwa Koirala ^b ,
Da Wei Li ^b ,
Chun Hu ^a

a 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;
b School of Pharmacy, Shanghai Jiao Tong University, Shanghai 300193, China

Received Date: 18 June 2010

Fund Project: This work was partially supported by the National Natural Science Foundation of China (NSFC) (No. 20474053).

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.
- Estrogen receptor antagonists,
- Synthesis,
- Biological activity,
- Thiophene,
- Pyrazole,
- Thiopyran,
- Piperazine
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