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 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
PDF Full-text Download PDF Full-Text [152 KB, uploaded 2 October 2008 11:53 CEST]
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

Article Statistics

Load and display the download statistics.

Citations to this Article

Cite This Article

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 KM, Magiatis P, Haroutounian SA. 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.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert