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
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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