Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands

被引：75

作者：

Shah, N

Scanlan, TS ^{[1
]}

机构：

[1] Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA 94143 USA

[2] Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA

[3] Univ Calif San Francisco, Grad Grp Biophys, San Francisco, CA 94143 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

glucocorticoid; nuclear receptor; ligand;

D O I：

10.1016/j.bmcl.2004.07.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of phenylpyrazole fused Wieland-Miescher ketone derivatives are high affinity, receptor specific, selective modulators of glucocorticoid receptor (GR) mediated transcription in vitro, dissociating transactivation, AP-1 repression, and NF-kappaB repression from each other. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5199 / 5203

页数：5

共 32 条

[1] Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor:: Receptor binding and in vivo activity [J].

Ali, A ;

Thompson, CF ;

Balkovec, JM ;

Graham, DW ;

Hammond, ML ;

Quraishi, N ;

Tata, JR ;

Einstein, M ;

Ge, L ;

Harris, G ;

Kelly, TM ;

Mazur, P ;

Pandit, S ;

Santoro, J ;

Sitlani, A ;

Wang, CL ;

Williamson, J ;

Miller, DK ;

Thompson, CM ;

Zaller, DM ;

Forrest, MJ ;

Carballo-Jane, E ;

Luell, S .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (10) :2441-2452

[2]

ALI A, 2002, Patent No. 03086294

[3] A proline-catalyzed asymmetric Robinson annulation reaction [J].

Bui, T ;

Barbas, CF .

TETRAHEDRON LETTERS, 2000, 41 (36) :6951-6954

[4] A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects [J].

Coghlan, MJ ;

Jacobson, PB ;

Lane, B ;

Nakane, M ;

Lin, CW ;

Elmore, SW ;

Kym, PR ;

Luly, JR ;

Carter, GW ;

Turner, R ;

Tyree, CM ;

Hu, JL ;

Elgort, M ;

Rosen, J ;

Miner, JN .

MOLECULAR ENDOCRINOLOGY, 2003, 17 (05) :860-869

[5] Structure and specificity of nuclear receptor-coactivator interactions [J].

Darimont, BD ;

Wagner, RL ;

Apriletti, JW ;

Stallcup, MR ;

Kushner, PJ ;

Baxter, JD ;

Fletterick, RJ ;

Yamamoto, KR .

GENES & DEVELOPMENT, 1998, 12 (21) :3343-3356

[6]

Davis G F, 1986, Clin Dermatol, V4, P161, DOI 10.1016/0738-081X(86)90020-9

[7] Nonsteroidal selective glucocorticoid modulators: The effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines [J].

Elmore, SW ;

Coghlan, MJ ;

Anderson, DD ;

Pratt, JK ;

Green, BE ;

Wang, AX ;

Stashko, MA ;

Lin, CW ;

Tyree, CM ;

Miner, JN ;

Jacobson, PB ;

Wilcox, DM ;

Lane, BC .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (25) :4481-4491

[8] SUBSTITUTED PYRAZOLO CORTICOIDS AS TOPICAL ANTIINFLAMMATORY AGENTS [J].

HANNAH, J ;

KELLY, K ;

PATCHETT, AA ;

STEELMAN, SL ;

MORGAN, ER .

JOURNAL OF MEDICINAL CHEMISTRY, 1975, 18 (02) :168-172

[9] Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors [J].

Hellal-Levy, C ;

Couette, B ;

Fagart, J ;

Souque, A ;

Gomez-Sanchez, C ;

Rafestin-Oblin, ME .

FEBS LETTERS, 1999, 464 (1-2) :9-13

[10] Cross-talk between glucocorticoid receptor and AP-1 [J].

Herrlich, P .

ONCOGENE, 2001, 20 (19) :2465-2475

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