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

Rui Sun, Jing Song, Hui Zhao, Chun-Li Yan, Ai-Jun Zhang, Diwa Koirala, Da-Wei Li, Chun Hu*   

  1. 1. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
    2. School of Pharmacy, Shanghai Jiao Tong University, Shanghai 300193, China
  • Received:2010-08-04 Revised:2010-10-15 Online:2011-01-15 Published:2011-01-15
  • Contact: Chun Hu*

Abstract:

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 antiproliferative 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.

Key words: Synthesis, 1,4-Dihydrothieno[3',2':5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives, Anti-tumor activity

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