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Synthesis of Novel Nitro-substituted Triaryl Pyrazole Derivatives as Potential Estrogen Receptor Ligands
- Source :
- Molecules, Vol 12, Iss 7, Pp 1259-1273 (2007), Molecules; Volume 12; Issue 7; Pages: 1259-1273
- Publication Year :
- 2007
- Publisher :
- MDPI AG, 2007.
-
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.
- Subjects :
- Stereochemistry
Substituent
Pharmaceutical Science
Estrogen receptor
Pyrazole
Ring (chemistry)
Ligands
Analytical Chemistry
lcsh:QD241-441
chemistry.chemical_compound
lcsh:Organic chemistry
Drug Discovery
Estrogen Receptor beta
Humans
Physical and Theoretical Chemistry
Estrogen receptor beta
Full Paper
Chemistry
Organic Chemistry
Estrogen Receptor alpha
Pyrazoles
SERMs
Estrogen Receptor Binding Affinity
Nitro Compounds
Chemistry (miscellaneous)
Nitro
Molecular Medicine
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 12
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....0406a6e8fd2317d1e611b98208915f55