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Page 1
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Pike KG, Morris J, Ruston L, Pass SL, Greenwood R, Williams EJ, Demeritt J, Culshaw JD, Gill K, Pass M, Finlay MR, Good CJ, Roberts CA, Currie GS, Blades K, Eden JM, Pearson SE. Pike KG, et al. Among authors: ruston l. J Med Chem. 2015 Mar 12;58(5):2326-49. doi: 10.1021/jm501778s. Epub 2015 Feb 18. J Med Chem. 2015. PMID: 25643210
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L. Addie M, et al. Among authors: ruston l. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.
Barlaam B, Cosulich S, Fitzek M, Germain H, Green S, Hanson LL, Harris CS, Hancox U, Hudson K, Lambert-van der Brempt C, Lamorlette M, Magnien F, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B. Barlaam B, et al. Among authors: ruston l. Bioorg Med Chem Lett. 2017 Jul 1;27(13):3030-3035. doi: 10.1016/j.bmcl.2017.05.028. Epub 2017 May 10. Bioorg Med Chem Lett. 2017. PMID: 28526367
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M. Grimster NP, et al. Among authors: ruston l. J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13. J Med Chem. 2018. PMID: 29856615
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.
Barlaam B, Cosulich S, Fitzek M, Green S, Harris CS, Hudson K, Lambert-van der Brempt C, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B. Barlaam B, et al. Among authors: ruston l. Bioorg Med Chem Lett. 2015 Jul 1;25(13):2679-85. doi: 10.1016/j.bmcl.2015.04.084. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25980912
Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
Barlaam B, Cosulich S, Delouvrié B, Ellston R, Fitzek M, Germain H, Green S, Hancox U, Harris CS, Hudson K, Lambert-van der Brempt C, Lebraud H, Magnien F, Lamorlette M, Le Griffon A, Morgentin R, Ouvry G, Page K, Pasquet G, Polanska U, Ruston L, Saleh T, Vautier M, Ward L. Barlaam B, et al. Among authors: ruston l. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62. doi: 10.1016/j.bmcl.2015.10.002. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26475521
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: ruston l. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
IMI - Oral biopharmaceutics tools project - Evaluation of bottom-up PBPK prediction success part 4: Prediction accuracy and software comparisons with improved data and modelling strategies.
Ahmad A, Pepin X, Aarons L, Wang Y, Darwich AS, Wood JM, Tannergren C, Karlsson E, Patterson C, Thörn H, Ruston L, Mattinson A, Carlert S, Berg S, Murphy D, Engman H, Laru J, Barker R, Flanagan T, Abrahamsson B, Budhdeo S, Franek F, Moir A, Hanisch G, Pathak SM, Turner D, Jamei M, Brown J, Good D, Vaidhyanathan S, Jackson C, Nicolas O, Beilles S, Nguefack JF, Louit G, Henrion L, Ollier C, Boulu L, Xu C, Heimbach T, Ren X, Lin W, Nguyen-Trung AT, Zhang J, He H, Wu F, Bolger MB, Mullin JM, van Osdol B, Szeto K, Korjamo T, Pappinen S, Tuunainen J, Zhu W, Xia B, Daublain P, Wong S, Varma MVS, Modi S, Schäfer KJ, Schmid K, Lloyd R, Patel A, Tistaert C, Bevernage J, Nguyen MA, Lindley D, Carr R, Rostami-Hodjegan A. Ahmad A, et al. Among authors: ruston l. Eur J Pharm Biopharm. 2020 Nov;156:50-63. doi: 10.1016/j.ejpb.2020.08.006. Epub 2020 Aug 14. Eur J Pharm Biopharm. 2020. PMID: 32805361
15 results