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Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Giordanetto F, Green S, Inghardt T, Hennequin L, Hancox U, Lambert-van der Brempt C, Morgentin R, Pass S, Plé P, Saleh T, Ward L. Barlaam B, et al. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3928-35. doi: 10.1016/j.bmcl.2014.06.040. Epub 2014 Jun 21. Bioorg Med Chem Lett. 2014. PMID: 24992874
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J. Boyd S, et al. Among authors: degorce sl. J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13. J Med Chem. 2015. PMID: 25849762
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Péru A, Plé P, Saleh T, Ward L, Warin N. Barlaam B, et al. Bioorg Med Chem Lett. 2016 May 1;26(9):2318-23. doi: 10.1016/j.bmcl.2016.03.034. Epub 2016 Mar 11. Bioorg Med Chem Lett. 2016. PMID: 26996374
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Ellston R, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Plé P, Ward L, Warin N. Barlaam B, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954. doi: 10.1016/j.bmcl.2017.03.027. Epub 2017 Mar 14. Bioorg Med Chem Lett. 2017. PMID: 28347666
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: degorce sl. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Degorce SL, Anjum R, Dillman KS, Drew L, Groombridge SD, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Scott JS, Stokes S, Xue Y. Degorce SL, et al. Bioorg Med Chem. 2018 Feb 15;26(4):913-924. doi: 10.1016/j.bmc.2018.01.008. Epub 2018 Jan 17. Bioorg Med Chem. 2018. PMID: 29398441
27 results