ERβ ligands.: Part 1:: The discovery of ERβ selective ligands which embrace the 4-hydroxy-biphenyl template

被引：67

作者：

Edsall, RJ

Harris, HA

Manas, ES

Mewshaw, RE

机构：

[1] Wyeth Ayerst Res, Chem & Screening Sci, Collegeville, PA 19426 USA

[2] Wyeth Ayerst Res, Womens Hlth Res Inst, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0968-0896(03)00303-1

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERP selectivity on the order of 20-70-fold. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：3457 / 3474

页数：18

相关论文

共 28 条

[1] The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site [J].

Anstead, GM ;

Carlson, KE ;

Katzenellenbogen, JA .

STEROIDS, 1997, 62 (03) :268-303

[2] Molecular basis of agonism and antagonism in the oestrogen receptor [J].

Brzozowski, AM ;

Pike, ACW ;

Dauter, Z ;

Hubbard, RE ;

Bonn, T ;

Engstrom, O ;

Ohman, L ;

Greene, GL ;

Gustafsson, JA ;

Carlquist, M .

NATURE, 1997, 389 (6652) :753-758

[3] CHARACTERIZATION AND COLOCALIZATION OF STEROID BINDING AND DIMERIZATION ACTIVITIES IN THE MOUSE ESTROGEN-RECEPTOR [J].

FAWELL, SE ;

LEES, JA ;

WHITE, R ;

PARKER, MG .

CELL, 1990, 60 (06) :953-962

[4] HUMAN ESTROGEN-RECEPTOR CDNA - SEQUENCE, EXPRESSION AND HOMOLOGY TO V-ERB-A [J].

GREEN, S ;

WALTER, P ;

KUMAR, V ;

KRUST, A ;

BORNERT, JM ;

ARGOS, P ;

CHAMBON, P .

NATURE, 1986, 320 (6058) :134-139

[5] SEQUENCE AND EXPRESSION OF HUMAN ESTROGEN-RECEPTOR COMPLEMENTARY-DNA [J].

GREENE, GL ;

GILNA, P ;

WATERFIELD, M ;

BAKER, A ;

HORT, Y ;

SHINE, J .

SCIENCE, 1986, 231 (4742) :1150-1154

[6] Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand [J].

Harris, HA ;

Katzenellenbogen, JA ;

Katzenellenbogen, BS .

ENDOCRINOLOGY, 2002, 143 (11) :4172-4177

[7] The ligand binding profiles of estrogen receptors α and β are species dependent [J].

Harris, HA ;

Bapat, AR ;

Gonder, DS ;

Frail, DE .

STEROIDS, 2002, 67 (05) :379-384

[8] A new series of estrogen receptor modulators that display selectivity for estrogen receptor β [J].

Henke, BR ;

Consler, TG ;

Go, N ;

Hale, RL ;

Hohman, DR ;

Jones, SA ;

Lu, AT ;

Moore, LB ;

Moore, JT ;

Orband-Miller, LA ;

Robinett, RG ;

Shearin, J ;

Spearing, PK ;

Stewart, EL ;

Turnbull, PS ;

Weaver, SL ;

Williams, SP ;

Wisely, GB ;

Lambert, MH .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (25) :5492-5505

[9] Biphenyls as potential mimetics of protein α-helix [J].

Jacoby, E .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (06) :891-893

[10]

KARIMONT BD, 1998, GENE DEV, V12, P3343