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    Bioorg Med Chem Lett. 2010 Feb 1;20(3):862-5. Epub 2009 Dec 28.

    Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase.

    Kocalka P, Rejman D, Vanek V, Rinnová M, Tomecková I, Králíková S, Petrová M, Páv O, Pohl R, Budesínský M, Liboska R, Tocík Z, Panova N, Votruba I, Rosenberg I.

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    Institute of Organic Chemistry and Biochemistry, Academy of Sciences vvi, Flemingovo 2, 166 10 Prague 6, Czech Republic.

    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 IC(50) values below 1 microM were selected. Out of them, four compounds strongly inhibited the enzyme with IC(50) values lying in a range of 11-45 nM. These most potent compounds might be bi-substrate analogues.

    Copyright (c) 2009 Elsevier Ltd. All rights reserved.

    PMID:
    20053558
    [PubMed - indexed for MEDLINE]

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