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Page 1
AiZynth impact on medicinal chemistry practice at AstraZeneca.
Shields JD, Howells R, Lamont G, Leilei Y, Madin A, Reimann CE, Rezaei H, Reuillon T, Smith B, Thomson C, Zheng Y, Ziegler RE. Shields JD, et al. RSC Med Chem. 2024 Feb 16;15(4):1085-1095. doi: 10.1039/d3md00651d. eCollection 2024 Apr 24. RSC Med Chem. 2024. PMID: 38665822
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. J Med Chem. 2014. PMID: 25271963
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.
McCoull W, Hennessy EJ, Blades K, Chuaqui C, Dowling JE, Ferguson AD, Goldberg FW, Howe N, Jones CR, Kemmitt PD, Lamont G, Varnes JG, Ward RA, Yang B. McCoull W, et al. ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. doi: 10.1021/acsmedchemlett.6b00322. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994749 Free PMC article.
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.
Kettle JG, Bagal SK, Barratt D, Bodnarchuk MS, Boyd S, Braybrooke E, Breed J, Cassar DJ, Cosulich S, Davies M, Davies NL, Deng C, Eatherton A, Evans L, Feron LJ, Fillery S, Gleave ES, Goldberg FW, Cortés González MA, Guerot C, Haider A, Harlfinger S, Howells R, Jackson A, Johnström P, Kemmitt PD, Koers A, Kondrashov M, Lamont GM, Lamont S, Lewis HJ, Liu L, Mylrea M, Nash S, Niedbala MJ, Peter A, Phillips C, Pike K, Raubo P, Robb GR, Ross S, Sanders MG, Schou M, Simpson I, Steward O. Kettle JG, et al. Among authors: lamont gm. J Med Chem. 2023 Jul 13;66(13):9147-9160. doi: 10.1021/acs.jmedchem.3c00746. Epub 2023 Jul 3. J Med Chem. 2023. PMID: 37395055
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
Smith JM, Barlaam B, Beattie D, Bradshaw L, Chan HM, Chiarparin E, Collingwood O, Cooke SL, Cronin A, Cumming I, Dean E, Debreczeni JÉ, Del Barco Barrantes I, Diene C, Gianni D, Guerot C, Guo X, Guven S, Hayhow TG, Hong T, Kemmitt PD, Lamont GM, Lamont S, Lynch JT, McWilliams L, Moore S, Raubo P, Robb GR, Robinson J, Scott JS, Srinivasan B, Steward O, Stubbs CJ, Syson K, Tan L, Turner O, Underwood E, Urosevic J, Vazquez-Chantada M, Whittaker AL, Wilson DM, Winter-Holt JJ. Smith JM, et al. Among authors: lamont gm. J Med Chem. 2024 Aug 22;67(16):13604-13638. doi: 10.1021/acs.jmedchem.4c00097. Epub 2024 Jul 30. J Med Chem. 2024. PMID: 39080842
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. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
20 results