Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

被引：42

作者：

Aubry, C

Wilson, AJ

Jenkins, PR ^{[1
]}

Mahale, S

Chaudhuri, B

Maréchal, JD

Sutcliffe, MJ

机构：

[1] Univ Leicester, Dept Chem, Leicester LE1 7RH, Leics, England

[2] De Montfort Univ, Sch Pharm, Leicester LE1 9BH, Leics, England

[3] Univ Leicester, Dept Biochem, Leicester LE1 7RH, Leics, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2006年 / 4卷 / 05期

关键词：

D O I：

10.1039/b518019h

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 mu M.

引用

页码：787 / 801

页数：15

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