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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,*
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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