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Page 1
Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.
Angibaud P, Arts J, Van Emelen K, Poncelet V, Pilatte I, Roux B, Van Brandt S, Verdonck M, De Winter H, Ten Holte P, Marien A, Floren W, Janssens B, Van Dun J, Aerts A, Van Gompel J, Gaurrand S, Queguiner L, Argoullon JM, Van Hijfte L, Freyne E, Janicot M. Angibaud P, et al. Among authors: van hijfte l, van gompel j, van dun j, van brandt s, van emelen k. Eur J Med Chem. 2005 Jun;40(6):597-606. doi: 10.1016/j.ejmech.2005.01.008. Epub 2005 Mar 3. Eur J Med Chem. 2005. PMID: 15922843
Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors.
Angibaud P, Van Emelen K, Decrane L, van Brandt S, Ten Holte P, Pilatte I, Roux B, Poncelet V, Speybrouck D, Queguiner L, Gaurrand S, Mariën A, Floren W, Janssen L, Verdonck M, van Dun J, van Gompel J, Gilissen R, Mackie C, Du Jardin M, Peeters J, Noppe M, Van Hijfte L, Freyne E, Page M, Janicot M, Arts J. Angibaud P, et al. Among authors: van hijfte l, van gompel j, van dun j, van brandt s, van emelen k. Bioorg Med Chem Lett. 2010 Jan 1;20(1):294-8. doi: 10.1016/j.bmcl.2009.10.118. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2010. PMID: 19906529
1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Rombouts FJ, Tresadern G, Delgado O, Martínez-Lamenca C, Van Gool M, García-Molina A, Alonso de Diego SA, Oehlrich D, Prokopcova H, Alonso JM, Austin N, Borghys H, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Alexander R, Macdonald G, Moechars D, Gijsen H, Trabanco AA. Rombouts FJ, et al. Among authors: van brandt s. J Med Chem. 2015 Oct 22;58(20):8216-35. doi: 10.1021/acs.jmedchem.5b01101. Epub 2015 Oct 10. J Med Chem. 2015. PMID: 26378740
Anilinotriazoles as potent gamma secretase modulators.
Velter AI, Bischoff FP, Berthelot D, De Cleyn M, Oehlrich D, Jaroskova L, Macdonald G, Minne G, Pieters S, Rombouts F, Van Brandt S, Van Roosbroeck Y, Surkyn M, Trabanco AA, Tresadern G, Wu T, Borghys H, Mercken M, Masungi C, Gijsen H. Velter AI, et al. Among authors: van roosbroeck y, van brandt s. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5805-5813. doi: 10.1016/j.bmcl.2014.10.024. Epub 2014 Oct 18. Bioorg Med Chem Lett. 2014. PMID: 25454273
Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.
Bischoff FP, Velter AI, Minne G, Pieters S, Berthelot D, De Cleyn M, Gijsen HJM, Macdonald G, Surkyn M, Van Brandt S, Van Roosbroeck Y, Zavattaro C, Mercken M, Austin N, Dhuyvetter D, Borghys H, Ahmad I, Samanta SK. Bischoff FP, et al. Among authors: van brandt s. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1737-1745. doi: 10.1016/j.bmcl.2019.05.023. Epub 2019 May 15. Bioorg Med Chem Lett. 2019. PMID: 31122869
Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martínez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Moechars D. Gijsen HJM, et al. Among authors: van brandt s. J Med Chem. 2018 Jun 28;61(12):5292-5303. doi: 10.1021/acs.jmedchem.8b00304. Epub 2018 Jun 11. J Med Chem. 2018. PMID: 29809004
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.
Oehlrich D, Rombouts FJ, Berthelot D, Bischoff FP, De Cleyn MA, Jaroskova L, Macdonald G, Mercken M, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter AI, Wu T, Gijsen HJ. Oehlrich D, et al. Among authors: van brandt s. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4794-800. doi: 10.1016/j.bmcl.2013.06.100. Epub 2013 Jul 11. Bioorg Med Chem Lett. 2013. PMID: 23890837
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Peschiulli A, Oehlrich D, Van Gool M, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Tresadern G, Rombouts FJR, Macdonald GJ, Moechars D, Trabanco AA, Gijsen HJM. Peschiulli A, et al. Among authors: van brandt s. ACS Med Chem Lett. 2021 Dec 1;13(1):76-83. doi: 10.1021/acsmedchemlett.1c00445. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059126 Free PMC article.
15 results