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Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter RN 3rd, Johnson JH, Knick VB, Laudeman CP, Luttrell DK, Mook RA, Nolte RT, Rudolph SK, Szewczyk JR, Truesdale AT, Veal JM, Wang L, Stafford JA. Harris PA, et al. J Med Chem. 2008 Aug 14;51(15):4632-40. doi: 10.1021/jm800566m. Epub 2008 Jul 12. J Med Chem. 2008. PMID: 18620382
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Cheung M, Harris PA, Badiang JG, Peckham GE, Chamberlain SD, Alberti MJ, Jung DK, Harris SS, Bramson NH, Epperly AH, Stimpson SA, Peel MR. Cheung M, et al. Among authors: harris pa, harris ss. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5428-30. doi: 10.1016/j.bmcl.2008.09.040. Epub 2008 Sep 12. Bioorg Med Chem Lett. 2008. PMID: 18818075
The discovery of potent cRaf1 kinase inhibitors.
Lackey K, Cory M, Davis R, Frye SV, Harris PA, Hunter RN, Jung DK, McDonald OB, McNutt RW, Peel MR, Rutkowske RD, Veal JM, Wood ER. Lackey K, et al. Among authors: harris pa. Bioorg Med Chem Lett. 2000 Feb 7;10(3):223-6. doi: 10.1016/s0960-894x(99)00668-x. Bioorg Med Chem Lett. 2000. PMID: 10698440
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Bramson HN, Corona J, Davis ST, Dickerson SH, Edelstein M, Frye SV, Gampe RT Jr, Harris PA, Hassell A, Holmes WD, Hunter RN, Lackey KE, Lovejoy B, Luzzio MJ, Montana V, Rocque WJ, Rusnak D, Shewchuk L, Veal JM, Walker DH, Kuyper LF. Bramson HN, et al. Among authors: harris pa. J Med Chem. 2001 Dec 6;44(25):4339-58. doi: 10.1021/jm010117d. J Med Chem. 2001. PMID: 11728181
Pyrazolo[1,5-a]pyridines as p38 kinase inhibitors.
Stevens KL, Jung DK, Alberti MJ, Badiang JG, Peckham GE, Veal JM, Cheung M, Harris PA, Chamberlain SD, Peel MR. Stevens KL, et al. Among authors: harris pa. Org Lett. 2005 Oct 13;7(21):4753-6. doi: 10.1021/ol0519745. Org Lett. 2005. PMID: 16209527
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM, Lehr R, Lich JD, Nagilla R, Nolte RT, Ouellette MT, Pao CS, Schaeffer MC, Smallwood A, Sun HH, Swift BA, Totoritis RD, Ward P, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. ACS Med Chem Lett. 2013 Nov 4;4(12):1238-43. doi: 10.1021/ml400382p. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900635 Free PMC article.
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. J Med Chem. 2016. PMID: 26854747
417 results