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Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Feb2010, Vol. 20 Issue 3, p862-865. 4p. - Publication Year :
- 2010
-
Abstract
- Abstract: 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 1μM were selected. Out of them, four compounds strongly inhibited the enzyme with IC50 values lying in a range of 11–45nM. These most potent compounds might be bi-substrate analogues. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 3
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 47949839
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.12.081