2,6,9-trisubstituted purines: Optimization towards highly potent and selective CDK1 inhibitors

被引：93

作者：

Imbach, P ^{[1
]}

Capraro, HG ^{[1
]}

Furet, P ^{[1
]}

Mett, H ^{[1
]}

Meyer, T ^{[1
]}

Zimmermann, J ^{[1
]}

机构：

[1] Novartis Ltd, Therapeut Area Oncol, Novartis Pharmaceut, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(98)00691-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described, (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：91 / 96

页数：6

共 29 条

[11] Combinatorial synthesis of 2,9-substituted purines. [J].

Gray, NS ;

Kwon, S ;

Schultz, PG .

TETRAHEDRON LETTERS, 1997, 38 (07) :1161-1164

[12] CELL-CYCLE REGULATION OF CDK2 ACTIVITY BY PHOSPHORYLATION OF THR160 AND TYR15 [J].

GU, Y ;

ROSENBLATT, J ;

MORGAN, DO .

EMBO JOURNAL, 1992, 11 (11) :3995-4005

[13] INHIBITION OF CDK2 ACTIVITY IN-VIVO BY AN ASSOCIATED 20K REGULATORY SUBUNIT [J].

GU, Y ;

TURCK, CW ;

MORGAN, DO .

NATURE, 1993, 366 (6456) :707-710

[14] Cytokinin-derived cyclin-dependent kinase inhibitors: Synthesis and cdc2 inhibitory activity of olomoucine and related compounds [J].

Havlicek, L ;

Hanus, J ;

Vesely, J ;

Leclerc, S ;

Meijer, L ;

Shaw, G ;

Strnad, M .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (04) :408-412

[15] Maturation promoting factor, cyclin and the control of M-phase [J].

Hunt, T. .

CURRENT OPINION IN CELL BIOLOGY, 1989, 1 (02) :268-274

[16]

KITAGAWA M, 1993, ONCOGENE, V8, P2425

[17] STUDIES ON THE ALKYLATION OF DERIVATIVES OF GUANINE [J].

KJELLBERG, J ;

JOHANSSON, NG .

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, 1989, 8 (02) :225-256

[18] Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases [J].

Legraverend, M ;

Ludwig, O ;

Bisagni, E ;

Leclerc, S ;

Meijer, L .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (07) :793-798

[19] Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5 [J].

Meijer, L ;

Borgne, A ;

Mulner, O ;

Chong, JPJ ;

Blow, JJ ;

Inagaki, N ;

Inagaki, M ;

Delcros, JG ;

Moulinoux, JP .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 1997, 243 (1-2) :527-536

[20] CYCLIN IS A COMPONENT OF THE SEA-URCHIN EGG M-PHASE SPECIFIC HISTONE H-1 KINASE [J].

MEIJER, L ;

ARION, D ;

GOLSTEYN, R ;

PINES, J ;

BRIZUELA, L ;

HUNT, T ;

BEACH, D .

EMBO JOURNAL, 1989, 8 (08) :2275-2282

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