1.
Bioorg Med Chem Lett
; 16(15): 3896-901, 2006 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-16730987
ABSTRACT
Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERbeta subtype selective ligands is described. Analogs possessing subnanomolar ERbeta binding, greater than 100-fold ERbeta-selectivity, and oral bioavailability are reported.
Subject(s)
Estrogen Receptor beta/drug effects , Fluorenes/chemistry , Pyrazoles/chemistry , Animals , Area Under Curve , Biological Availability , Cyclization , Estrogen Receptor beta/metabolism , Fluorenes/blood , Fluorenes/metabolism , Rats
2.
Bioorg Med Chem Lett
; 16(13): 3489-94, 2006 Jul 01.
Article
in English
| MEDLINE
| ID: mdl-16632357
ABSTRACT
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
Subject(s)
Estrogen Receptor beta/drug effects , Fluorenes/chemical synthesis , Fluorenes/pharmacology , Cell Line , Crystallography, X-Ray , Estrogen Receptor alpha/chemistry , Estrogen Receptor alpha/drug effects , Estrogen Receptor beta/chemistry , Fluorenes/classification , Humans , Ligands , Models, Molecular , Molecular Structure , Stereoisomerism , Structure-Activity Relationship
3.
Comput Nurs
; 6(6): 244-52, 1988.
Article
in English
| MEDLINE
| ID: mdl-3072999
4.
Bull Med Libr Assoc
; 73(2): 210-2, 1985 Apr.
Article
in English
| MEDLINE
| ID: mdl-2581646