Výsledky vyhledávání - "Sara Van Poecke"

Synthesis of 5-Substituted 2′-Deoxyuridine-5′- Phosphonate Analogues and Evaluation of their Antiviral Activity

Autor: José C. Martins, Jan Balzarini, Serge Van Calenbergh, Davy Sinnaeve, Sara Van Poecke

Publikováno v: NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

A small series of 5-(hetero)aryl-modified nucleoside phosphonates was synthesized via an 8-step procedure including a Wittig reaction and Suzuki-Miyaura coupling. An unanticipated anomerization during phosphonate deprotection allowed us to isolate bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1fee6c6aa34d199928e07393d836d69
https://doi.org/10.1080/15257770.2012.654876

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Synthesis, modeling and evaluation of 3′-(1-aryl-1H-tetrazol-5-ylamino)-substituted 3′-deoxythymidine derivatives as potent and selective human mitochondrial thymidine kinase inhibitors

Autor: Anna Karlsson, Andrea Negri, Nicola Solaroli, Jan Balzarini, Federico Gago, Sara Van Poecke, Serge Van Calenbergh, Jolien Janssens

Publikováno v: Org. Biomol. Chem.. 9:892-901

Based on the presumed binding mode of an earlier identified inhibitor, we herein report new 3'-modified nucleosides as potent and selective inhibitors of mitochondrial thymidine kinase (TK2). A series of thirteen 3'-amino-, 3'-guanidino- and 3'-tetra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0d7e532139c51bf86f8ba8c5150f1ff
https://doi.org/10.1039/c0ob00591f

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3′-[4-Aryl-(1,2,3-triazol-1-yl)]-3′-deoxythymidine Analogues as Potent and Selective Inhibitors of Human Mitochondrial Thymidine Kinase

Autor: Ineke Van Daele, Serge Van Calenbergh, Anna Karlsson, Federico Gago, Nicola Solaroli, Jan Balzarini, Andrea Negri, Sara Van Poecke

Publikováno v: JOURNAL OF MEDICINAL CHEMISTRY

In an effort to increase the potency and selectivity of earlier identified substrate-based inhibitors of mitochondrial thymidine kinase 2 (TK-2), we now describe the synthesis of new thymidine analogues containing a 4- or 5-substituted 1,2,3-triazol-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::524ee7c1c700d6f2d41f28dd309ecd6f
https://doi.org/10.1021/jm901532h

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Synthesis and P2Y2 receptor agonist activities of uridine 5′-phosphonate analogues

Autor: Davy Sinnaeve, Kenneth A. Jacobson, Sara Van Poecke, José C. Martins, T. Kendall Harden, Serge Van Calenbergh, T. Santhosh Kumar, Matthew O. Barrett

We explored the influence of modifications of uridine 5'-methylenephosphonate on biological activity at the human P2Y(2) receptor. Key steps in the synthesis of a series of 5-substituted uridine 5'-methylenephosphonates were the reaction of a suitabl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ac83b6cbb70eb4dfe7fa91ec73f3176

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Synthesis and P2Y₂ receptor agonist activities of uridine 5'-phosphonate analogues

Autor: Sara, Van Poecke, Matthew O, Barrett, T, Santhosh Kumar, Davy, Sinnaeve, José C, Martins, Kenneth A, Jacobson, T, Kendall Harden, Serge, Van Calenbergh

Publikováno v: Bioorganicmedicinal chemistry. 20(7)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::435484e2810d6de65a297f547bd4aa81
https://pubmed.ncbi.nlm.nih.gov/22386981

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Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase

Autor: Sara Van Poecke, Olivier Helynck, Matheus Froeyen, Serge Van Calenbergh, Hélène Munier-Lehmann

Publikováno v: Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry, Elsevier, 2011, 19, epub ahead of print. ⟨10.1016/j.bmc.2011.10.021⟩
Bioorganic and Medicinal Chemistry, 2011, 19, epub ahead of print. ⟨10.1016/j.bmc.2011.10.021⟩
BIOORGANIC & MEDICINAL CHEMISTRY

International audience; We report on Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitory activities of a series of new 3'- and 5'-modified thymidine analogues including α- and β-derivatives. In addition, several analogues

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60ec6d050492d2a3a7e4ddb92baa2b22
https://hal-pasteur.archives-ouvertes.fr/pasteur-00645423

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Synthesis of base-substituted uridine 5'-phosphonate analogues as potential P2Y2 receptor ligands

Autor: T. Kendall Harden, Serge Van Calenbergh, Matthew O. Barrett, Kenneth A. Jacobson, Sara Van Poecke

Publikováno v: Collection Symposium

A series of 5-modified 5’-phosphonate derivatives of UMP has been prepared in 6 steps from uridine. The analogs were evaluated for their affinity at the P2Y2 receptor. Several derivatives showed partial agonistic activity at the P2Y2 receptor.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54c937f27ec3b6ee4dff0e4478bcf8e3
https://hdl.handle.net/1854/LU-4390040

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Synthesis of α-Substituted Fosmidomycin Analogues as Highly Potent Plasmodium falciparum Growth Inhibitors

Autor: Timothy Haemers, Sara Van Poecke, Hassan Jomaa, Edwald Beck, Dajana Henschker, Jan Goeman, Jochen Wiesner, Serge Van Calenbergh

Publikováno v: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In view of the promising antimalarial activity of fosmidomycin or its N-acetyl homologue FR900098, the objective of this work was to investigate the influence of aromatic substituents in the α-position of the phosphonate moiety. The envisaged analog

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::142632d94718cf32679179926e7db63d
https://doi.org/10.1002/chin.200628199

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From M-tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitors towards mitochondrial thymidine kinase (TK-2) inhibitors

Autor: Jan Balzarini, Sara Van Poecke, Hélene Munier Lehmann, Matheus Froeyen, Serge Van Calenbergh, Ineke Van Daele

Publikováno v: ResearcherID

Here, we report on the enzyme structure-aided design of a series of substituted 3'- or 5'-thiourea derivatives of beta- and alpha-thymidine, respectively, as thymidine monophosphate kinase inhibitors of M. tuberculosis. In a recent study, several 3'-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::959d48f78bf2fb0078887c8d5b775b31
http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=ORCID&SrcApp=OrcidOrg&DestLinkType=FullRecord&DestApp=WOS_CPL&KeyUT=WOS:000257885700011&KeyUID=WOS:000257885700011

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