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

Authors :
Wilkening RR
Ratcliffe RW
Tynebor EC
Wildonger KJ
Fried AK
Hammond ML
Mosley RT
Fitzgerald PM
Sharma N
McKeever BM
Nilsson S
Carlquist M
Thorsell A
Locco L
Katz R
Frisch K
Birzin ET
Wilkinson HA
Mitra S
Cai S
Hayes EC
Schaeffer JM
Rohrer SP
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Jul 01; Vol. 16 (13), pp. 3489-94. Date of Electronic Publication: 2006 May 02.
Publication Year :
2006

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.

Details

Language :
English
ISSN :
0960-894X
Volume :
16
Issue :
13
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
16632357
Full Text :
https://doi.org/10.1016/j.bmcl.2006.03.098