From M-tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitors towards mitochondrial thymidine kinase (TK-2) inhibitors

被引：0

作者：

Van Calenbergh, Serge ^{[1
]}

Van Daele, Ineke ^{[1
]}

Van Poecke, Sara ^{[1
]}

Froeyen, Matheus

Lehmann, Helene Munier

Balzarini, Jan

机构：

[1] Univ Ghent, Lab Med Chem FFW, B-9000 Ghent, Belgium

来源：

CHEMISTRY OF NUCLEIC ACID COMPONENTS | 2008年 / 10卷

关键词：

D O I：

暂无

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：

Here, we report on the enzyme structure-aided design of a series of substituted 3'- or 5'-thiourea derivatives of beta- and alpha-thymidine, respectively, as thymidine monophosphate kinase inhibitors of M. tuberculosis. In a recent study, several 3'-thiourea substituted thymidine derivatives were found to be exquisitely potent and specific inhibitors of mitochondrial thymidine kinase (TK-2), with high selectivity when compared with cytosolic TK-1.

引用

页码：87 / 93

页数：7

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