Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

被引：105

作者：

Beauchard, Anne

Ferandin, Yoan

Frere, Stephane

Lozach, Olivier

Blairvacq, Melina

Meijer, Laurent

Thiery, Valerie

Besson, Thierry

机构：

[1] Univ La Rochelle, UFR Sci Fondamentales & Sci Ingn, FRE 2766, CNRS,Lab Biotechnol & Chim Bioorgan, F-17042 La Rochelle, France

[2] Cell Cycle Grp, UMR 7150, F-29682 Roscoff, France

[3] UPS2682, Biol Stn, F-29682 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 18期

关键词：

indirubin; cyclin-dependent kinase; glycogen synthase kinase-3;

D O I：

10.1016/j.bmc.2006.05.036

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：

In an effort to identify new pharmacological inhibitors of disease-relevant protein kinases with increased potency and selectivity, we synthesized and evaluated new 5-substituted indirubins. The effects of 34 indirubin derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3, as well as on SH-SY5Y human neuroblastoma cell survival, were investigated. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6434 / 6443

页数：10

共 22 条

[1]

BESSON T, 2006, TOPICS HETEROCYCLIC

[2] Sequential dephosphorylation of p34(cdc2) on Thr-14 and Tyr-15 at the prophase/metaphase transition [J].

Borgne, A ;

Meijer, L .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (44) :27847-27854

[3] Tyrian purple:: 6,6′-dibromoindigo and related compounds [J].

Cooksey, CJ .

MOLECULES, 2001, 6 (09) :736-769

[4] Anti-mitotic properties of indirubin-3'-monoxime, a CDK/GSK-3 inhibitor: induction of endoreplication following prophase arrest [J].

Damiens, E ;

Baratte, B ;

Marie, D ;

Eisenbrand, G ;

Meijer, L .

ONCOGENE, 2001, 20 (29) :3786-3797

[5] Inhibition of cyclin-dependent kinases by purine analogues - Crystal structure of human cdk2 complexed with roscovitine [J].

DeAzevedo, WF ;

Leclerc, S ;

Meijer, L ;

Havlicek, L ;

Strnad, M ;

Kim, SH .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 1997, 243 (1-2) :518-526

[6] The design of drug candidate molecules as selective inhibitors of therapeutically relevant protein kinases [J].

Fischer, PM .

CURRENT MEDICINAL CHEMISTRY, 2004, 11 (12) :1563-1583

[7] Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases [J].

Hoessel, R ;

Leclerc, S ;

Endicott, JA ;

Nobel, MEM ;

Lawrie, A ;

Tunnah, P ;

Leost, M ;

Damiens, E ;

Marie, D ;

Marko, D ;

Niederberger, E ;

Tang, WC ;

Eisenbrand, G ;

Meijer, L .

NATURE CELL BIOLOGY, 1999, 1 (01) :60-67

[8] Controlled microwave heating in modern organic synthesis [J].

Kappe, CO .

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2004, 43 (46) :6250-6284

[9] Pharmacological inhibitors of cyclin-dependent kinases [J].

Knockaert, M ;

Greengard, P ;

Meijer, L .

TRENDS IN PHARMACOLOGICAL SCIENCES, 2002, 23 (09) :417-425

[10] Indirubins inhibit glycogen synthase kinase-3β and CDK5/P25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease -: A property common to most cycline-dependent kinase inhibitors? [J].

Leclerc, S ;

Garnier, M ;

Hoessel, R ;

Marko, D ;

Bibb, JA ;

Snyder, GL ;

Greengard, P ;

Biernat, J ;

Wu, YZ ;

Mandelkow, EM ;

Eisenbrand, G ;

Meijer, L .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (01) :251-260

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