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Bioorg Med Chem Lett ; 18(12): 3628-31, 2008 Jun 15.
Article in English | MEDLINE | ID: mdl-18513963

ABSTRACT

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.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Thiazolidines/chemical synthesis , Thiazolidines/pharmacology , Thymidylate Synthase/antagonists & inhibitors , Drug Design , Drug Evaluation, Preclinical , Enzyme Inhibitors/chemistry , Molecular Conformation , Stereoisomerism , Structure-Activity Relationship , Thiazolidines/chemistry , Thymidylate Synthase/chemistry , Time Factors
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