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Page 1
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT. Johnson CN, et al. Among authors: freyne ej. ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589925 Free PMC article.
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT. Johnson CN, et al. Among authors: freyne ej. ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589926 Free PMC article.
Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV. Perera TPS, et al. Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24. Mol Cancer Ther. 2017. PMID: 28341788
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. 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
Synthesis and biological evaluation of 1,2,4-triazinylphenylalkylthiazolecarboxylic acid esters as cytokine-inhibiting antedrugs with strong bronchodilating effects in an animal model of asthma.
Freyne EJ, Lacrampe JF, Deroose F, Boeckx GM, Willems M, Embrechts W, Coesemans E, Willems JJ, Fortin JM, Ligney Y, Dillen LL, Cools WF, Goossens J, Corens D, De Groot A, Van Wauwe JP. Freyne EJ, et al. J Med Chem. 2005 Mar 24;48(6):2167-75. doi: 10.1021/jm049479m. J Med Chem. 2005. PMID: 15771459
Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.
Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT. Squires M, et al. Among authors: freyne e. Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15. Mol Cancer Ther. 2011. PMID: 21764904
Design and synthesis of a series of piperazine-1-carboxamidine derivatives with antifungal activity resulting from accumulation of endogenous reactive oxygen species.
François IE, Thevissen K, Pellens K, Meert EM, Heeres J, Freyne E, Coesemans E, Viellevoye M, Deroose F, Martinez Gonzalez S, Pastor J, Corens D, Meerpoel L, Borgers M, Ausma J, Dispersyn GD, Cammue BP. François IE, et al. ChemMedChem. 2009 Oct;4(10):1714-21. doi: 10.1002/cmdc.200900249. ChemMedChem. 2009. PMID: 19705386
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Andrés JI, Alonso JM, Díaz A, Fernández J, Iturrino L, Martínez P, Matesanz E, Freyne EJ, Deroose F, Boeckx G, Petit D, Diels G, Megens A, Somers M, Van Wauwe J, Stoppie P, Cools M, De Clerck F, Peeters D, de Chaffoy D. Andrés JI, et al. Among authors: freyne ej. Bioorg Med Chem Lett. 2002 Feb 25;12(4):653-8. doi: 10.1016/s0960-894x(01)00817-4. Bioorg Med Chem Lett. 2002. PMID: 11844693
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Angibaud P, Bourdrez X, End DW, Freyne E, Janicot M, Lezouret P, Ligny Y, Mannens G, Damsch S, Mevellec L, Meyer C, Muller P, Pilatte I, Poncelet V, Roux B, Smets G, Van Dun J, Van Remoortere P, Venet M, Wouters W. Angibaud P, et al. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4365-9. doi: 10.1016/j.bmcl.2003.08.080. Bioorg Med Chem Lett. 2003. PMID: 14643327
21 results