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4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA. Liddle J, et al. Among authors: williamson ra. Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19349179
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: williamson ra. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).
Christopher JA, Bamborough P, Alder C, Campbell A, Cutler GJ, Down K, Hamadi AM, Jolly AM, Kerns JK, Lucas FS, Mellor GW, Miller DD, Morse MA, Pancholi KD, Rumsey W, Solanke YE, Williamson R. Christopher JA, et al. J Med Chem. 2009 May 14;52(9):3098-102. doi: 10.1021/jm9000117. J Med Chem. 2009. PMID: 19348415
The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in rats as a measure of emetogenicity.
Davis TG, Peterson JJ, Kou JP, Capper-Spudich EA, Ball D, Nials AT, Wiseman J, Solanke YE, Lucas FS, Williamson RA, Ferrari L, Wren P, Knowles RG, Barnette MS, Podolin PL. Davis TG, et al. Among authors: williamson ra. J Pharmacol Exp Ther. 2009 Sep;330(3):922-31. doi: 10.1124/jpet.109.152454. Epub 2009 Jun 4. J Pharmacol Exp Ther. 2009. PMID: 19498103
282 results