期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 3, 页码 862-865出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.081
关键词
Phosphonate; Pyrrolidine; Nucleotide analogues; Thymidine phosphorylase; Rat T-cell lymphomas
资金
- Czech Science Foundation [203/09/0820, 202/09/0193]
- Ministry of Education, CR [LC06061, LC06077, 2B06065]
- Acad. Sci. CR [KAN200520801, QS400550501]
- Ministry of Health of the Czech Republic [NR/9138-3, Z40550506]
Structurally diverse, sugar-modified, thymine-containing nucleoside phosphonic acids were evaluated for their ability to inhibit thymidine phosphorylase (TP, EC 2.4.2.4) purified from spontaneous T-cell lymphomas of an inbred Sprague-Dawley rat strain. From a large set of tested compounds, among them a number of pyrrolidine-based derivatives, 10 nucleotide analogues with IC50 values below 1 mu M were selected. Out of them, four compounds strongly inhibited the enzyme with IC50 values lying in a range of 11-45 nM. These most potent compounds might be bi-substrate analogues. (C) 2009 Elsevier Ltd. All rights reserved.
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