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Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.
Crosignani S, Bingham P, Bottemanne P, Cannelle H, Cauwenberghs S, Cordonnier M, Dalvie D, Deroose F, Feng JL, Gomes B, Greasley S, Kaiser SE, Kraus M, Négrerie M, Maegley K, Miller N, Murray BW, Schneider M, Soloweij J, Stewart AE, Tumang J, Torti VR, Van Den Eynde B, Wythes M. Crosignani S, et al. Among authors: deroose f. J Med Chem. 2017 Dec 14;60(23):9617-9629. doi: 10.1021/acs.jmedchem.7b00974. Epub 2017 Nov 21. J Med Chem. 2017. PMID: 29111717
In vivo inhibition of RIPK2 kinase alleviates inflammatory disease.
Tigno-Aranjuez JT, Benderitter P, Rombouts F, Deroose F, Bai X, Mattioli B, Cominelli F, Pizarro TT, Hoflack J, Abbott DW. Tigno-Aranjuez JT, et al. Among authors: deroose f. J Biol Chem. 2014 Oct 24;289(43):29651-64. doi: 10.1074/jbc.M114.591388. Epub 2014 Sep 11. J Biol Chem. 2014. PMID: 25213858 Free PMC article.
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. Among authors: deroose f. J Med Chem. 2005 Mar 24;48(6):2167-75. doi: 10.1021/jm049479m. J Med Chem. 2005. PMID: 15771459
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: deroose f. 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
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. Among authors: deroose f. ChemMedChem. 2009 Oct;4(10):1714-21. doi: 10.1002/cmdc.200900249. ChemMedChem. 2009. PMID: 19705386
Synthesis of 3-amino-4-fluoropyrazoles.
Surmont R, Verniest G, De Schrijver M, Thuring JW, ten Holte P, Deroose F, De Kimpe N. Surmont R, et al. Among authors: deroose f. J Org Chem. 2011 May 20;76(10):4105-11. doi: 10.1021/jo2000989. Epub 2011 Apr 29. J Org Chem. 2011. PMID: 21500813
New synthesis of 3-fluoropyrroles.
Surmont R, Verniest G, Colpaert F, Macdonald G, Thuring JW, Deroose F, De Kimpe N. Surmont R, et al. Among authors: deroose f. J Org Chem. 2009 Feb 6;74(3):1377-80. doi: 10.1021/jo802272n. J Org Chem. 2009. PMID: 19115927
Synthesis of 1-Boc-3-fluoroazetidine-3-carboxylic acid.
Van Hende E, Verniest G, Deroose F, Thuring JW, Macdonald G, De Kimpe N. Van Hende E, et al. Among authors: deroose f. J Org Chem. 2009 Mar 6;74(5):2250-3. doi: 10.1021/jo802791r. J Org Chem. 2009. PMID: 19216497
Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles.
Williamson AE, Ylioja PM, Robertson MN, Antonova-Koch Y, Avery V, Baell JB, Batchu H, Batra S, Burrows JN, Bhattacharyya S, Calderon F, Charman SA, Clark J, Crespo B, Dean M, Debbert SL, Delves M, Dennis AS, Deroose F, Duffy S, Fletcher S, Giaever G, Hallyburton I, Gamo FJ, Gebbia M, Guy RK, Hungerford Z, Kirk K, Lafuente-Monasterio MJ, Lee A, Meister S, Nislow C, Overington JP, Papadatos G, Patiny L, Pham J, Ralph SA, Ruecker A, Ryan E, Southan C, Srivastava K, Swain C, Tarnowski MJ, Thomson P, Turner P, Wallace IM, Wells TN, White K, White L, Willis P, Winzeler EA, Wittlin S, Todd MH. Williamson AE, et al. Among authors: deroose f. ACS Cent Sci. 2016 Oct 26;2(10):687-701. doi: 10.1021/acscentsci.6b00086. Epub 2016 Sep 14. ACS Cent Sci. 2016. PMID: 27800551 Free PMC article.
14 results