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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: shen mwh. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Identification and optimization of indolo[2,3-c]quinoline inhibitors of IRAK4.
Tumey LN, Boschelli DH, Bhagirath N, Shim J, Murphy EA, Goodwin D, Bennett EM, Wang M, Lin LL, Press B, Shen M, Frisbie RK, Morgan P, Mohan S, Shin J, Rao VR. Tumey LN, et al. Bioorg Med Chem Lett. 2014 May 1;24(9):2066-72. doi: 10.1016/j.bmcl.2014.03.056. Epub 2014 Mar 29. Bioorg Med Chem Lett. 2014. PMID: 24726805
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Lee KL, Foley MA, Chen L, Behnke ML, Lovering FE, Kirincich SJ, Wang W, Shim J, Tam S, Shen MW, Khor S, Xu X, Goodwin DG, Ramarao MK, Nickerson-Nutter C, Donahue F, Ku MS, Clark JD, McKew JC. Lee KL, et al. J Med Chem. 2007 Mar 22;50(6):1380-400. doi: 10.1021/jm061131z. Epub 2007 Feb 17. J Med Chem. 2007. PMID: 17305324
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization.
McKew JC, Foley MA, Thakker P, Behnke ML, Lovering FE, Sum FW, Tam S, Wu K, Shen MW, Zhang W, Gonzalez M, Liu S, Mahadevan A, Sard H, Khor SP, Clark JD. McKew JC, et al. J Med Chem. 2006 Jan 12;49(1):135-58. doi: 10.1021/jm0507882. J Med Chem. 2006. PMID: 16392799
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
15 results