Synthesis and biological activity of olomoucine II

被引：60

作者：

Krystof, V

Lenobel, R

Havlícek, L

Kuzma, M

Strnad, M

机构：

[1] Palacky Univ, Lab Growth Regulators, Olomouc 78371, Czech Republic

[2] VF Kuprevich Expt Bot Inst, Olomouc 78371, Czech Republic

[3] Acad Sci Czech Republ, Isotope Lab, Inst Expt Bot, Prague 14220 4, Czech Republic

[4] Acad Sci Czech Republ, Inst Microbiol, CR-14220 Prague 4, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(02)00693-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on our previous experiences with synthesis of purines, novel 2,6,9-trisubstituted purine derivatives were prepared and assayed for the ability to inhibit CDK1/cyclin B kinase. One of newly synthesized compounds designated as olomoucine II, 6-[(2-hydroxybenzyl)amino]-2-{[1-(hydroxymethyl)propyl]amino}-9-isopropylpurine, displays 10 times higher inhibitory activity than roscovitine, potent and specific CDK1 inhibitor. Olomoucine 11 in vitro cytotoxic activity exceeds purvalanol A, the most potent CDK inhibitor, as it kills the CEM cells with IC50 value of 3.0 muM. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：3283 / 3286

页数：4

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