6-Substituted 5-fluorouracil derivatives as transition state analogue inhibitors of thymidine phosphorylase

被引：13

作者：

Kalman, TI ^{[1
]}

Lai, L ^{[1
]}

机构：

[1] SUNY Buffalo, Dept Chem, Buffalo, NY 14260 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2005年 / 24卷 / 5-7期

关键词：

D O I：

10.1081/NCN-200059790

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A combination of mechanism-based and structure-based design strategies led to the synthesis of a series of 5 and 6-substituted uracil derivatives as potential inhibitors of thymidine phosphorlase/platelet derived endothelial cell growth factor (TP/PD-ECGF). Among those tested, 6-imidazoolmethyl-5-fluorouracil was found to be the most potent inhibitor with a K-i-value of 51 nM, representing a new class of 5-fluoropyrimidines with a novel mechanism of action.

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页码：367 / 373

页数：7

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