Synthesis of Novel Nitro-substituted Triaryl Pyrazole Derivatives as Potential Estrogen Receptor LigandsReport as inadecuate




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1

Chemistry Laboratory, Agricultural University of Athens, Iera odos 75, Athens 11855, Greece

2

Faculty of Pharmacy, Laboratory of Pharmacognosy and Natural Products Chemistry, University of Athens, Panepistimiopolis Zografou, Athens 15771, Greece





*

Author to whom correspondence should be addressed.



Abstract Novel tetrasubstituted pyrazole derivatives bearing a nitro substituent on their A-phenol ring were synthesized and their binding affinity towards the estrogen receptor ER subtypes ERα and ERβ was determined. Among compounds tested, the 2-nitrophenol derivative 5c was found to bind satisfactorily to both estrogen receptor subtypes RBAα=5.17 and RBAβ=3.27. In general, the introduction of a nitro group into the A ring of these compounds was found to benefit their ERβ binding abilities. View Full-Text

Keywords: Pyrazoles; SERMs; Estrogen Receptor Binding Affinity Pyrazoles; SERMs; Estrogen Receptor Binding Affinity





Author: Fotini Naoum 1, Konstantinos M Kasiotis 1, Prokopios Magiatis 2 and Serkos A Haroutounian 1,*

Source: http://mdpi.com/



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