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新型5,6-二取代尿嘧啶衍生物作为胸苷磷酸化酶强效抑制剂的设计与合成

Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.

作者信息

Nencka Radim, Votruba Ivan, Hrebabecký Hubert, Tloust'ová Eva, Horská Kveta, Masojídková Milena, Holý Antonín

机构信息

Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 166 10 Prague 6, Czech Republic.

出版信息

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. doi: 10.1016/j.bmcl.2005.11.050. Epub 2005 Dec 5.

DOI:10.1016/j.bmcl.2005.11.050
PMID:16337119
Abstract

We report on a series of novel 5,6-disubstituted uracils with significant inhibitory activity against human and Escherichia coli thymidine phosphorylases. Bis-uracil conjugates were identified as the most potent inhibitors of TPs in this study.

摘要

我们报道了一系列对人和大肠杆菌胸苷磷酸化酶具有显著抑制活性的新型5,6-二取代尿嘧啶。在本研究中,双尿嘧啶缀合物被确定为胸苷磷酸化酶最有效的抑制剂。

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