Thymidine and thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Autor: Philippe Van Rompaey, Veerle Vanheusden, Sylvie Pochet, Serge Van Calenbergh, Piet Herdewijn, Hélène Munier-Lehmann

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2003, 13 (18), pp.3045-8. ⟨10.1016/S0960-894X(03)00643-7⟩
Bioorganic and Medicinal Chemistry Letters, 2003, 13 (18), pp.3045-8. ⟨10.1016/S0960-894X(03)00643-7⟩

International audience; The affinity of a series of 2', 3'- and 5-modified thymidine analogues for Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) was evaluated. The affinities of several non-phosphorylated analogues are in the sam

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43f38fe2a9e1ffde7d9d3bf3e771049d
https://doi.org/10.1016/s0960-894x(03)00643-7

Synthesis and evaluation of thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Autor: Piet Herdewijn, Serge Van Calenbergh, Sylvie Pochet, Veerle Vanheusden, Hélène Munier-Lehmann

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, 2002, 12 (19), pp.2695-8. ⟨10.1016/S0960-894X(02)00551-6⟩
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2002, 12 (19), pp.2695-8. ⟨10.1016/S0960-894X(02)00551-6⟩

International audience; A number of 2'- and 3'-modified thymidine 5'-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::787134b41dca92e7b2e380dcbca1edc9
https://doi.org/10.1016/s0960-894x(02)00551-6

Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

Autor: Serge Van Calenbergh, Piet Herdewijn, Jef Rozenski, Veerle Vanheusden, Roger Busson, Hélène Munier-Lehmann, Matheus Froeyen

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 2004, 47 (25), pp.6187-94. ⟨10.1021/jm040847w⟩
Journal of Medicinal Chemistry, American Chemical Society, 2004, 47 (25), pp.6187-94. ⟨10.1021/jm040847w⟩
JOURNAL OF MEDICINAL CHEMISTRY

International audience; Thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for selectively blocking bacterial DNA synthesis. Hereby, we report on the discovery of a novel class of bicyclic nucleoside

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b3fadad5956f83e6538d4a2eaa1e749
https://hal-pasteur.archives-ouvertes.fr/pasteur-00166959

Mycobacterium tuberculosis thymidine monophosphate kinase inhibitors: Biological evaluation and conformational analysis of 2 '- and 3 '-modified thymidine analogues

Autor: Veerle Vanheusden, Philippe Van Rompaey, Piet Herdewijn, Koen Nauwelaerts, Jef Rozenski, Hélène Munier-Lehmann, Serge Van Calenbergh

Publikováno v: European Journal of Organic Chemistry
European Journal of Organic Chemistry, Wiley-VCH Verlag, 2003, 15, pp.2911-2918. ⟨10.1002/ejoc.200300177⟩
European Journal of Organic Chemistry, 2003, 15, pp.2911-2918. ⟨10.1002/ejoc.200300177⟩
Scopus-Elsevier
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) has recently been introduced as a potential target for the structure-based design of anti-tuberculosis drugs. Based on the TMPKmt X-ray structure and previous S.A.R. studies, we synth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bad37a9bc65138ecf64f686f3dea291f
https://hal-pasteur.archives-ouvertes.fr/pasteur-00167037

3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

Autor: Veerle Vanheusden, Serge Van Calenbergh, Roger Busson, Sylvie Pochet, Arne Heyerick, Hélène Munier-Lehmann, Denis De Keukeleire, Laurence Dugué, Piet Herdewijn, Matheus Froeyen

Publikováno v: JOURNAL OF MEDICINAL CHEMISTRY
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2003, 46 (18), pp.3811-21. ⟨10.1021/jm021108n⟩
Journal of Medicinal Chemistry, 2003, 46 (18), pp.3811-21. ⟨10.1021/jm021108n⟩

International audience; Thymidine monophosphate kinase (TMPK) of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for blocking the bacterial DNA synthesis. In an attempt to find high-affinity inhibitors of TMPKmt, a cavity in the e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3b8e2fb6d88ba9794ea067c15064098
https://hdl.handle.net/1854/LU-209651