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Page 1
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, Grist M, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Ward RA, et al. Among authors: dakin la. J Med Chem. 2013 Sep 12;56(17):7025-48. doi: 10.1021/jm400822z. Epub 2013 Aug 30. J Med Chem. 2013. PMID: 23930994
Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors.
Cowen SD, Russell D, Dakin LA, Chen H, Larsen NA, Godin R, Throner S, Zheng X, Molina A, Wu J, Cheung T, Howard T, Garcia-Arenas R, Keen N, Pendleton CS, Pietenpol JA, Ferguson AD. Cowen SD, et al. Among authors: dakin la. J Med Chem. 2016 Dec 22;59(24):11079-11097. doi: 10.1021/acs.jmedchem.6b01303. Epub 2016 Dec 1. J Med Chem. 2016. PMID: 28002961
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Gingipalli L, Block MH, Bao L, Cooke E, Dakin LA, Denz CR, Ferguson AD, Johannes JW, Larsen NA, Lyne PD, Pontz TW, Wang T, Wu X, Wu A, Zhang HJ, Zheng X, Dowling JE, Lamb ML. Gingipalli L, et al. Among authors: dakin la. Bioorg Med Chem Lett. 2018 May 1;28(8):1336-1341. doi: 10.1016/j.bmcl.2018.03.018. Epub 2018 Mar 7. Bioorg Med Chem Lett. 2018. PMID: 29559278
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Lyne PD, Aquila B, Cook DJ, Dakin LA, Ezhuthachan J, Ioannidis S, Pontz T, Su M, Ye Q, Zheng X, Block MH, Cowen S, Deegan TL, Lee JW, Scott DA, Custeau D, Drew L, Poondru S, Shen M, Wu A. Lyne PD, et al. Among authors: dakin la. Bioorg Med Chem Lett. 2009 Feb 1;19(3):1026-9. doi: 10.1016/j.bmcl.2008.10.053. Epub 2008 Oct 15. Bioorg Med Chem Lett. 2009. PMID: 19097792
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Dakin LA, Block MH, Chen H, Code E, Dowling JE, Feng X, Ferguson AD, Green I, Hird AW, Howard T, Keeton EK, Lamb ML, Lyne PD, Pollard H, Read J, Wu AJ, Zhang T, Zheng X. Dakin LA, et al. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. doi: 10.1016/j.bmcl.2012.05.098. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22727640
3-amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor.
Scott DA, Dakin LA, Del Valle DJ, Diebold RB, Drew L, Gero TW, Ogoe CA, Omer CA, Repik G, Thakur K, Ye Q, Zheng X. Scott DA, et al. Among authors: dakin la. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1382-4. doi: 10.1016/j.bmcl.2011.01.033. Epub 2011 Jan 14. Bioorg Med Chem Lett. 2011. PMID: 21295474
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ. Vaswani RG, et al. Among authors: dakin la. J Med Chem. 2016 Nov 10;59(21):9928-9941. doi: 10.1021/acs.jmedchem.6b01315. Epub 2016 Oct 28. J Med Chem. 2016. PMID: 27739677 Free PMC article.
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Yang B, Hird AW, Bodnarchuk MS, Zheng X, Dakin L, Su Q, Daly K, Godin R, Hattersley MM, Brassil P, Redmond S, John Russell D, Janetka JW. Yang B, et al. Bioorg Med Chem. 2020 Jan 15;28(2):115227. doi: 10.1016/j.bmc.2019.115227. Epub 2019 Dec 11. Bioorg Med Chem. 2020. PMID: 31862310
29 results