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Synthesis and evaluation of 5'-modified thymidines and 5-hydroxymethyl-2'-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors.

Abstract : We report the synthesis of 5'-modified thymidines (16, 18, 21, 23) and 5,5'-bis-substituted 2'-deoxyuridine analogues (30, 47) as inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt). These analogues were evaluated for their capacity to inhibit TMPKmt and solely two 5'-modified thymidines were found to possess moderate inhibitory activity. In addition, a feasibility study of protecting groups for the 5-CH(2)OH moiety of 2'-deoxyuridines is described that enables to introduce the desired 5'-modification.
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https://hal-pasteur.archives-ouvertes.fr/pasteur-00849837
Contributor : Hélène Munier-Lehmann <>
Submitted on : Thursday, August 1, 2013 - 11:28:55 AM
Last modification on : Monday, January 13, 2020 - 5:08:16 PM

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Kiran S Toti, Frederick Verbeke, Martijn D P Risseeuw, Vladimir Frecer, Hélène Munier-Lehmann, et al.. Synthesis and evaluation of 5'-modified thymidines and 5-hydroxymethyl-2'-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors.. Bioorganic and Medicinal Chemistry, Elsevier, 2013, 21 (1), pp.257-68. ⟨10.1016/j.bmc.2012.10.018⟩. ⟨pasteur-00849837⟩

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