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

收藏

页码：793 / 798

页数：6

相关论文

共 14 条

[1] 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

[2]

DUNPHY WG, 1997, METHODS ENZYMOLOGY C, V283, P678

[3] PALLADIUM-CATALYZED REACTIONS OF ORGANIC HALIDES WITH OLEFINS [J].

HECK, RF .

ACCOUNTS OF CHEMICAL RESEARCH, 1979, 12 (04) :146-151

[4]

KOYAMA S, 1982, NUCLEIC ACIDS S SERI, V11, P41

[5] Regiochemistry in Stille couplings of 2,6-dihalopurines [J].

Langli, G ;

Gundersen, LL ;

Rise, F .

TETRAHEDRON, 1996, 52 (15) :5625-5638

[6] SYNTHESIS OF NEW (+/-)-3,5-DIHYDROXYPENTYL NUCLEOSIDE ANALOGS FROM 1-AMINO-5-(BENZYLOXY)PENTAN-3-OL AND THEIR ANTIVIRAL EVALUATION [J].

LEGRAVEREND, M ;

BOUMCHITA, H ;

ZERIAL, A ;

HUEL, C ;

LEMAITRE, M ;

BISAGNI, E .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (09) :2476-2480

[7] NUCLEOSIDES AND NUCLEOTIDES .103. 2-ALKYNYLADENOSINES - A NOVEL CLASS OF SELECTIVE ADENOSINE-A2 RECEPTOR AGONISTS WITH POTENT ANTIHYPERTENSIVE EFFECTS [J].

MATSUDA, A ;

SHINOZAKI, M ;

YAMAGUCHI, T ;

HOMMA, H ;

NOMOTO, R ;

MIYASAKA, T ;

WATANABE, Y ;

ABIRU, T .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (02) :241-252

[8] 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

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

Meijer, L .

TRENDS IN CELL BIOLOGY, 1996, 6 (10) :393-397

[10]

MEIJER L, 1997, PROGR CELL RES, V3