Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands.

Article Details

Citation

Naoum F, Kasiotis KM, Magiatis P, Haroutounian SA

Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands.

Molecules. 2007 Jul 2;12(7):1259-73.

PubMed ID
17909483 [ View in PubMed
]
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 ERalpha and ERbeta was determined. Among compounds tested, the 2-nitrophenol derivative 5c was found to bind satisfactorily to both estrogen receptor subtypes (RBAalpha=5.17 and RBAbeta=3.27). In general, the introduction of a nitro group into the A ring of these compounds was found to benefit their ERbeta binding abilities.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
PyrazoleEstrogen receptor alphaProteinHumans
Unknown
Not AvailableDetails
PyrazoleEstrogen receptor betaProteinHumans
Unknown
Not AvailableDetails