PHOSPHONATE DERIVATIVES OF N9-BENZYLGUANINE - A NEW CLASS OF POTENT PURINE NUCLEOSIDE PHOSPHORYLASE INHIBITORS

被引：23

作者：

HALAZY, S ^{[1
]}

EGGENSPILLER, A ^{[1
]}

EHRHARD, A ^{[1
]}

DANZIN, C ^{[1
]}

机构：

[1] MARION MERRELL DOW RES INST,BP 447 R-9,16 RUE ANKARA,F-67009 STRASBOURG,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)80157-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New phosphonate derivatives of N-9-benzylguanine (5a - 5d) have been designed and prepared as purine nucleoside phosphorylase inhibitors. Enzyme inhibition studies with PNP from calf spleen or human erythrocytes demonstrate that the trifluorophosphonate 5b, the fluorovinylphosphonate 5c and the vinylphosphonate 5d, with K(i) values around 1 nM, are the most potent inhibitors of PNP ever reported.

引用

页码：407 / 410

页数：4

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