Medicinal Chemistry

Dimitra Hadjipavlou-Litina
Aristotle University of Thessaloniki
Thessaloniki
Greece

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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, Chun Hu.

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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: 8
Year: 2014
Page: [836 - 842]
Pages: 7
DOI: 10.2174/1573406410666140428145753
Price: $58