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Page 1
Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors.
Veerman JJN, Bruseker YB, Damen E, Heijne EH, van Bruggen W, Hekking KFW, Winkel R, Hupp CD, Keefe AD, Liu J, Thomson HA, Zhang Y, Cuozzo JW, McRiner AJ, Mulvihill MJ, van Rijnsbergen P, Zech B, Renzetti LM, Babiss L, Müller G. Veerman JJN, et al. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562. doi: 10.1021/acsmedchemlett.0c00547. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33859795 Free PMC article.
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R. Blaazer AR, et al. Among authors: veerman jjn. J Med Chem. 2018 May 10;61(9):3870-3888. doi: 10.1021/acs.jmedchem.7b01670. Epub 2018 May 1. J Med Chem. 2018. PMID: 29672041 Free PMC article.
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.
de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, Siderius M, de Esch IJP, Brown DG, Leurs R. de Heuvel E, et al. Bioorg Med Chem. 2019 Sep 15;27(18):3998-4012. doi: 10.1016/j.bmc.2019.06.027. Epub 2019 Jun 18. Bioorg Med Chem. 2019. PMID: 31327675 Free article.
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, Zorg S, Veerman J, Seebeck T, Sterk GJ, de Esch IJ, Leurs R. Orrling KM, et al. J Med Chem. 2012 Oct 25;55(20):8745-56. doi: 10.1021/jm301059b. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22963052