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The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.

Wilkening, R R; Ratcliffe, R W; Tynebor, E C; Wildonger, K J; Fried, A K; Hammond, M L; Mosley, R T; Fitzgerald, P M D; Sharma, N; McKeever, B M; Nilsson, S; Carlquist, M; Thorsell, A; Locco, L; Katz, R; Frisch, K; Birzin, E T; Wilkinson, H A; Mitra, S; Cai, S; Hayes, E C; Schaeffer, J M; Rohrer, S P.

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

The PDB format, mmCIF, and other data formats.

Westbrook, John D; Fitzgerald, P M D.

Methods Biochem Anal ; 44: 161-79, 2003.

Article in English | MEDLINE | ID: mdl-12647386

Subject(s)

Databases, Protein , Computational Biology , Crystallography, X-Ray , Dictionaries, Chemical as Topic , Macromolecular Substances , Molecular Structure

ABSTRACT

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