- The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
Bioorganic & medicinal chemistry letters (2006-04-25)
R R Wilkening, R W Ratcliffe, E C Tynebor, K J Wildonger, A K Fried, M L Hammond, R T Mosley, P M D Fitzgerald, N Sharma, B M McKeever, S Nilsson, M Carlquist, A Thorsell, L Locco, R Katz, K Frisch, E T Birzin, H A Wilkinson, S Mitra, S Cai, E C Hayes, J M Schaeffer, S P Rohrer
PMID16632357
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.