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Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T. Oubrie A, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):613-8. doi: 10.1016/j.bmcl.2011.10.071. Epub 2011 Nov 3. Bioorg Med Chem Lett. 2012. PMID: 22119462
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Kaptein A, Oubrie A, de Zwart E, Hoogenboom N, de Wit J, van de Kar B, van Hoek M, Vogel G, de Kimpe V, Schultz-Fademrecht C, Borsboom J, van Zeeland M, Versteegh J, Kazemier B, de Roos J, Wijnands F, Dulos J, Jaeger M, Leandro-Garcia P, Barf T. Kaptein A, et al. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3823-7. doi: 10.1016/j.bmcl.2011.04.016. Epub 2011 Apr 16. Bioorg Med Chem Lett. 2011. PMID: 21565498
Structure-based lead identification of ATP-competitive MK2 inhibitors.
Barf T, Kaptein A, de Wilde S, van der Heijden R, van Someren R, Demont D, Schultz-Fademrecht C, Versteegh J, van Zeeland M, Seegers N, Kazemier B, van de Kar B, van Hoek M, de Roos J, Klop H, Smeets R, Hofstra C, Hornberg J, Oubrie A. Barf T, et al. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3818-22. doi: 10.1016/j.bmcl.2011.04.018. Epub 2011 Apr 16. Bioorg Med Chem Lett. 2011. PMID: 21565500
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P. Ferrigno F, et al. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5. doi: 10.1016/j.bmcl.2009.11.087. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 20022747
35 results