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

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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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, Dan-Ni Wang, Diwa Koirala, Da-Wei Li and Chun Hu

Affiliation: Key Laboratory of Structure- Based Drug Design & Discovery, Ministry of Education, China, Shenyang Pharmaceutical University, Shenyang 110016, China.

Abstract

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.

Keywords: Anti-tumor activity, heterocycle, docking, synthesis.

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Article Details

Volume: 10
Issue Number: 8
First Page: 836
Last Page: 842
Page Count: 7
DOI: 10.2174/1573406410666140428145753
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