Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases

被引：50

作者：

Legraverend, M

Ludwig, O

Bisagni, E

Leclerc, S

Meijer, L

机构：

[1] Ctr Univ Orsay, Inst Curie, UMR 176 CNRS, F-91405 Orsay, France

[2] CNRS, Biol Stn, F-29682 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00097-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a new family of inhibitors of the cell cycle regulating cyclin-dependent kinases (CDK's) is reported. These compounds, related to the purines olomoucine and roscovitine, are characterised by the presence of alkynylated side chains at C2. They inhibit CDK's with IC50's in the 200 nM range. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：793 / 798

页数：6

共 14 条

[11] NAIR V, 1982, SYNTHESIS-STUTTGART, P670
[12] A structure-based library approach to kinase inhibitors
Norman, TC
Gray, NS
Koh, JT
Schultz, PG
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (31) : 7430 - 7431
[13] MULTIPLE-MODES OF LIGAND RECOGNITION - CRYSTAL-STRUCTURES OF CYCLIN-DEPENDENT PROTEIN-KINASE-2 IN COMPLEX WITH ATP AND 2 INHIBITORS, OLOMOUCINE AND ISOPENTENYLADENINE
SCHULZEGAHMEN, U
BRANDSEN, J
JONES, HD
MORGAN, DO
MEIJER, L
VESELY, J
KIM, SH
[J]. PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS, 1995, 22 (04) : 378 - 391
[14] INHIBITION OF CYCLIN-DEPENDENT KINASES BY PURINE ANALOGS
VESELY, J
HAVLICEK, L
STRNAD, M
BLOW, JJ
DONELLADEANA, A
PINNA, L
LETHAM, DS
KATO, J
DETIVAUD, L
LECLERC, S
MEIJER, L
[J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1994, 224 (02): : 771 - 786

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