Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines

被引：25

作者：

Hamann, LG

Winn, DT

Pooley, CLF

Tegley, CM

West, SJ

Farmer, LJ

Zhi, L

Edwards, JP

Marschke, KB

Mais, DE

Goldman, ME

Jones, TK

机构：

[1] Ligand Pharmaceut Inc, Dept Med Chem, San Diego, CA 92121 USA

[2] Ligand Pharmaceut Inc, Dept New Leads Discovery, San Diego, CA 92121 USA

[3] Ligand Pharmaceut Inc, Dept Endocrine Res, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00482-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells, (C) 1998 Elsevier Science Ltd. AU rights reserved.

引用

收藏

页码：2731 / 2736

页数：6

相关论文

共 24 条

[1] Induction of a novel conformation in the progesterone receptor by ZK299 involves a defined region of the carboxyl-terminal tail [J].

Allan, GF ;

Lombardi, E ;

HaynesJohnson, D ;

Palmer, S ;

Kiddoe, M ;

Kraft, P ;

Campen, C ;

Rybczynski, P ;

Combs, DW ;

Phillips, A .

MOLECULAR ENDOCRINOLOGY, 1996, 10 (10) :1206-1213

[2] INTERACTION OF GLUCOCORTICOID ANALOGS WITH THE HUMAN GLUCOCORTICOID RECEPTOR [J].

BERGER, TS ;

PARANDOOSH, Z ;

PERRY, BW ;

STEIN, RB .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1992, 41 (3-8) :733-738

[3]

BIGSBY RM, 1990, ATLA-ALTERN LAB ANIM, V18, P301

[4] NONSTEROIDAL PROGESTERONE-RECEPTOR LIGANDS .2. HIGH-AFFINITY LIGANDS WITH SELECTIVITY FOR BONE CELL PROGESTERONE RECEPTORS [J].

COMBS, DW ;

REESE, K ;

CORNELIUS, LAM ;

GUNNET, JW ;

CRYAN, EV ;

GRANGER, KS ;

JORDAN, JJ ;

DEMAREST, KT .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (25) :4880-4884

[5] NONSTEROIDAL PROGESTERONE-RECEPTOR LIGANDS .1. 3-ARYL-1-BENZOYL-1,4,5,6-TETRAHYDROPYRIDAZINES [J].

COMBS, DW ;

REESE, K ;

PHILLIPS, A .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (25) :4878-4879

[6]

Connolly PJ, 1997, BIOORG MED CHEM LETT, V7, P2551, DOI 10.1016/S0960-894X(97)10016-6

[7] 5-aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists:: The effect of D-ring substituents [J].

Edwards, JP ;

West, SJ ;

Marschke, KB ;

Mais, DE ;

Gottardis, MM ;

Jones, TK .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (03) :303-310

[8] Preparation, resolution, and biological evaluation of 5-aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines:: Potent, orally active, nonsteroidal progesterone receptor agonists [J].

Edwards, JP ;

Zhi, L ;

Pooley, CLF ;

Tegley, CM ;

West, SJ ;

Wang, MW ;

Gottardis, MM ;

Pathirana, C ;

Schrader, WT ;

Jones, TK .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (15) :2779-2785

[9] REARRANGEMENTS OF HETEROCYCLIC-COMPOUNDS .6. MECHANISM OF THE SKRAUP AND DOEBNER-VONMILLER QUINOLINE SYNTHESES - CYCLIZATION OF ALPHA,BETA-UNSATURATED N-ARYLIMINIUM SALTS VIA 1,3-DIAZETIDINIUM ION INTERMEDIATES [J].

EISCH, JJ ;

DLUZNIEWSKI, T .

JOURNAL OF ORGANIC CHEMISTRY, 1989, 54 (06) :1269-1274

[10] Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether [J].

Hamann, LG ;

Farmer, LJ ;

Johnson, MG ;

Bender, SL ;

Mais, DE ;

Wang, MW ;

Crombie, D ;

Goldman, ME ;

Jones, TK .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (09) :1778-1789