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

doi:10.3390/12071259

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

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

Fotini Naoum ¹, Konstantinos M. Kasiotis ¹, Prokopios Magiatis ² and Serkos A. Haroutounian 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; in revised form: 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

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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.

AMA 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(7):1259-1273.

Chicago/Turabian Style

Naoum, Fotini; Kasiotis, Konstantinos M.; Magiatis, Prokopios; Haroutounian, Serkos A. 2007. "Synthesis of Novel Nitro-substituted Triaryl Pyrazole Derivatives as Potential Estrogen Receptor Ligands." Molecules 12, no. 7: 1259-1273.

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