Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1

Autor: Adrian Hall, Jan Abendroth, Madison J. Bolejack, Tom Ceska, Sylvie Dell’Aiera, Victoria Ellis, David Fox, Cyril François, Muigai M. Muruthi, Camille Prével, Karine Poullennec, Sergei Romanov, Anne Valade, Alain Vanbellinghen, Jason Yano, Martine Geraerts

Publikováno v: ACS Medicinal Chemistry Letters. 13:1099-1108

We describe the identification and characterization of a series of covalent inhibitors of the C-terminal kinase domain (CTKD) of MSK1. The initial hit was identified via a high-throughput screening and represents a rare example of a covalent inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3a0207a67876bf40c7c83d5e98d0f32
https://doi.org/10.1021/acsmedchemlett.2c00134

Acetamide Scanning around Bicyclic Thiazoles: SAR at the H3 Receptor

Autor: Laurent Provins, Michel Gillard, Christel Delaunoy, Frédéric Denonne, Sabine Defays, Jean-Marie Nicolas, Geneviève Lorent, Eric Detrait, Véronique Durieu, Bernard Christophe, Yves Lamberty, Alain Vanbellinghen, Nathalie Van houtvin, Sylvain Celanire, Marie-Laure Delporte

Publikováno v: ChemMedChem. 6:1559-1565

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d838126cb62c79dcc6d4c0028d307312
https://doi.org/10.1002/cmdc.201100248

Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3Receptor (H3R) Inverse Agonists

Autor: Iwan J. P. de Esch, Yves Lamberty, Patrice Talaga, Valérie Verbois, Rob Leurs, Frédéric Denonne, Florence Lebon, Alain Vanbellinghen, Bernard Christophe, Michel Gillard, Christel Delaunoy, Sylvain Celanire, Edith Gelens, Erwin Snip, Henk Timmerman, Donald Dassesse, Nathalie Van houtvin, Laurent Provins, Benedicte Lallemand, Véronique Durieu, Philippe Collart, Jean-Marie Nicolas, Maikel Wijtmans, Luc Quere

Publikováno v: ChemMedChem, 4(7), 1063-8. John Wiley and Sons Ltd
Celanire, S, Wijtmans, M, Christophe, B, Collart, P, de Esch, I J P, Dassesse, D, Delaunoy, C, Denonne, F, Durieu, V, Gelens, E, Gillard, M, Lallemand, B, Lamberty, Y, Lebon, F, Nicolas, J M, Quere, L, Snip, E, Vanbellinghen, A, Van Houtvin, N, Verbois, V, Timmerman, H, Talaga, P, Leurs, R & Provins, L 2009, ' Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists ', ChemMedChem, vol. 4, no. 7, pp. 1063-8 . https://doi.org/10.1002/cmdc.200900055

H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::543d6a72ee98e4081c29c96d0b654379
https://doi.org/10.1002/cmdc.200900055