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Bioorg Med Chem Lett. 2008 Jun 15;18(12):3628-31. doi: 10.1016/j.bmcl.2008.04.080. Epub 2008 May 6.

Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.

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  • 1Unité de Pharmacologie Chimique et Génétique, Ecole Nationale Supérieure de Chimie de Paris, Paris, France.


Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.

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