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2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.
Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, Winter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SM, Berthelot DJ, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz AB. Baxter EW, et al. Among authors: berthelot dj. J Med Chem. 2007 Sep 6;50(18):4261-4. doi: 10.1021/jm0705408. Epub 2007 Aug 8. J Med Chem. 2007. PMID: 17685503
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: berthelot d. 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
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: berthelot d. 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: berthelot d. 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
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.
Pande V, Sun W, Beke L, Berthelot D, Brehmer D, Brown D, Corbera J, Irving S, Meerpoel L, Nys T, Parade M, Robinson C, Sommen C, Viellevoye M, Wu T, Thuring JW. Pande V, et al. Among authors: berthelot d. ACS Med Chem Lett. 2020 Sep 28;11(11):2227-2231. doi: 10.1021/acsmedchemlett.0c00355. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214833 Free PMC article.
Iron-Catalyzed Synthesis of Sulfur-Containing Heterocycles.
Bosset C, Lefebvre G, Angibaud P, Stansfield I, Meerpoel L, Berthelot D, Guérinot A, Cossy J. Bosset C, et al. Among authors: berthelot d. J Org Chem. 2017 Apr 21;82(8):4020-4036. doi: 10.1021/acs.joc.6b01827. Epub 2016 Oct 13. J Org Chem. 2017. PMID: 27736056
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