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

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

1, 1, 2 and 1,*
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.
Received: 11 June 2007 / Revised: 29 June 2007 / Accepted: 29 June 2007 / Published: 2 July 2007
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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.
Keywords: Pyrazoles; SERMs; Estrogen Receptor Binding Affinity Pyrazoles; SERMs; Estrogen Receptor Binding Affinity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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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