Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase.

作者信息

Pomeisl Karel, Holý Antonín, Votruba Ivan, Pohl Radek

机构信息

Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i, Centre for New Antivirals and Antineoplastics (IOCB), Prague, Czech Republic.

出版信息

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1364-7. doi: 10.1016/j.bmcl.2008.01.006. Epub 2008 Jan 8.

DOI:10.1016/j.bmcl.2008.01.006

PMID:18221873

Abstract

A series of N(3)-substituted thymine acyclic nucleoside phosphonates bearing a number of (phosphonomethoxy)alkyl groups were synthesized and investigated for their ability to inhibit the human thymidine phosphorylase expressed in V79 Chinese hamster cells, as well as thymidine phosphorylase from SD-lymphoma, Escherichia coli and human placenta. In comparison to N(1)- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed a marginal inhibitory effect of these compounds. None of the presented N(3)-substituted derivatives possess a significant cytostatic activity.

摘要

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