Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors

被引：13

作者：

Bapma, A

Vickerstaffe, E

Warrington, BH

Ladlow, M

Fan, TPD

Ley, SV

机构：

[1] Univ Cambridge, Dept Pharmacol, Cambridge CB2 1QJ, England

[2] Univ Cambridge, Chem Lab, GlaxoSmithKline Cambridge Technol Ctr, Cambridge CB2 1EW, England

[3] Univ Cambridge, Chem Lab, Dept Chem, Cambridge CB2 1EW, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2004年 / 2卷 / 04期

关键词：

D O I：

10.1039/b313414h

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The polymer-assisted solution phase synthesis (PASP) of an array of historic deacetylase (HDAc) inhibitors is described. HDAc inhibitors have considerable potential as new anti-proliferative agents. Selected compounds were shown to inhibit both human endothelial cell proliferation, and the formation of tubules (neovascularisation) in an in vitro model of angiogenesis.

引用

页码：611 / 620

页数：10

共 48 条

[21] Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation [J].

Jung, M ;

Brosch, G ;

Kölle, D ;

Scherf, H ;

Gerhäuser, C ;

Loidl, P .

JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (22) :4669-4679

[22] Histone deacetylases induce angiogenesis by negative regulation of tumor suppressor genes [J].

Kim, MS ;

Kwon, HJ ;

Lee, YM ;

Baek, JH ;

Jang, JE ;

Lee, SW ;

Moon, EJ ;

Kim, HS ;

Lee, SK ;

Chung, HY ;

Kim, CW ;

Kim, KW .

NATURE MEDICINE, 2001, 7 (04) :437-443

[23]

Kirschning A, 2001, ANGEW CHEM INT EDIT, V40, P650, DOI 10.1002/1521-3773(20010216)40:4<650::AID-ANIE6500>3.0.CO

[24]

2-C

[25] Acetylation: a regulatory modification to rival phosphorylation? [J].

Kouzarides, T .

EMBO JOURNAL, 2000, 19 (06) :1176-1179

[26] Histone deacetylase as a therapeutic target [J].

Krämer, OH ;

Göttlicher, M ;

Heinzel, T .

TRENDS IN ENDOCRINOLOGY AND METABOLISM, 2001, 12 (07) :294-300

[27] Design and synthesis of a novel class of histone deacetylase inhibitors [J].

Lavoie, R ;

Bouchain, G ;

Frechette, S ;

Woo, SH ;

Abou Khalil, E ;

Leit, S ;

Fournel, M ;

Yan, PT ;

Trachy-Bourget, MC ;

Beaulieu, C ;

Li, ZM ;

Besterman, J ;

Delorme, D .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (21) :2847-2850

[28] Use of polymer supported reagents for clean multi-step organic synthesis:: preparation of amines and amine derivatives from alcohols for use in compound library generation [J].

Ley, SV ;

Bolli, MH ;

Hinzen, B ;

Gervois, AG ;

Hall, BJ .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1998, (15) :2239-2241

[29] Polyurea-encapsulated palladium(II) acetate: a robust and recyclable catalyst for use in conventional and supercritical media [J].

Ley, SV ;

Ramarao, C ;

Gordon, RS ;

Holmes, AB ;

Morrison, AJ ;

McConvey, IF ;

Shirley, IM ;

Smith, SC ;

Smith, MD .

CHEMICAL COMMUNICATIONS, 2002, (10) :1134-1135

[30] Multi-step organic synthesis using solid-supported reagents and scavengers: a new paradigm in chemical library generation [J].

Ley, SV ;

Baxendale, IR ;

Bream, RN ;

Jackson, PS ;

Leach, AG ;

Longbottom, DA ;

Nesi, M ;

Scott, JS ;

Storer, RI ;

Taylor, SJ .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 2000, (23) :3815-4195

← 1 2 3 4 5 →