title: Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands.
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.
authors.affiliation: Chemistry Laboratory, Agricultural University of Athens, Iera odos 75, Athens 11855, Greece.
authors.forename: Fotini
authors.initials: F
authors.lastname: Naoum
authors.forename: Konstantinos M
authors.initials: KM
authors.lastname: Kasiotis
authors.forename: Prokopios
authors.initials: P
authors.lastname: Magiatis
authors.forename: Serkos A
authors.initials: SA
authors.lastname: Haroutounian
mesh_terms: D047628:Estrogen Receptor alpha / Q000378:metabolism*; D047629:Estrogen Receptor beta / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D009574:Nitro Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands; D009574:Nitro Compounds; D011720:Pyrazoles; C031280:pyrazole