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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
Epub Full Text Article
DOI: 10.2174/1573406410666140428145753      Price:  $95

Development of Thieno[3’,2’:5,6]thiopyrano[4,3-c]pyrazole-3-carboxamide Derivatives as the Estrogen Receptor Ligands: Synthesis, Characterization and Biological Activity

Author(s): Xin Wang, Rui Sun, Yushu Huang, Yisi Yan, Miaomiao Gao, Wang Dan-Ni, Diwa Koirala, Li Da-Wei and Chun Hu
Estrogen receptors (ERs) are members of a superfamily of ligand-modulated nuclear receptors, which have been associated with an increased risk of cardiovascular diseases and breast cancer. Based on molecular docking studies, 1,4-dihydrothieno[3’,2’:5,6]thiopyrano[4,3-c]pyrazole-3-carboxamide derivatives as estrogen receptor inhibitors with a new scaffold , have been synthesized and tested for the antitumor activity on the ER expressing (ER dependent) human MCF-7 breast cancer cell line. According to the biological activity evaluation, compound 6a demonstrated the most potent antiproliferative activity (relative inhibitory rate: 100%). Several of these compounds exhibited moderate antitumor activity and worthy of further modification to obtain more potent anticancer candidate drugs
Anti-tumor activity, Heterocycle, Docking, Synthesis
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, China; Shenyang Pharmaceutical University, Shenyang 110016, China