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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.

Authors :
Wang X
Sun R
Huang Y
Yan Y
Gao M
Wang DN
Koirala D
Li DW
Hu C
Source :
Medicinal chemistry (Shariqah (United Arab Emirates)) [Med Chem] 2014; Vol. 10 (8), pp. 836-42.
Publication Year :
2014

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.

Details

Language :
English
ISSN :
1875-6638
Volume :
10
Issue :
8
Database :
MEDLINE
Journal :
Medicinal chemistry (Shariqah (United Arab Emirates))
Publication Type :
Academic Journal
Accession number :
24773350
Full Text :
https://doi.org/10.2174/1573406410666140428145753