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Molecules 2007, 12(7), 1259-1273; doi:10.3390/12071259

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

Chemistry Laboratory, Agricultural University of Athens, Iera odos 75, Athens 11855, Greece
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.
Received: 11 June 2007 / Revised: 29 June 2007 / Accepted: 29 June 2007 / Published: 2 July 2007
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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

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MDPI and ACS Style

Naoum, F.; Kasiotis, K.M.; Magiatis, P.; Haroutounian, S.A. Synthesis of Novel Nitro-substituted Triaryl Pyrazole Derivatives as Potential Estrogen Receptor Ligands. Molecules 2007, 12, 1259-1273.

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