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Page 1
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
Tsou HR, Overbeek-Klumpers EG, Hallett WA, Reich MF, Floyd MB, Johnson BD, Michalak RS, Nilakantan R, Discafani C, Golas J, Rabindran SK, Shen R, Shi X, Wang YF, Upeslacis J, Wissner A. Tsou HR, et al. Among authors: floyd mb. J Med Chem. 2005 Feb 24;48(4):1107-31. doi: 10.1021/jm040159c. J Med Chem. 2005. PMID: 15715478
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Wissner A, Overbeek E, Reich MF, Floyd MB, Johnson BD, Mamuya N, Rosfjord EC, Discafani C, Davis R, Shi X, Rabindran SK, Gruber BC, Ye F, Hallett WA, Nilakantan R, Shen R, Wang YF, Greenberger LM, Tsou HR. Wissner A, et al. Among authors: floyd mb. J Med Chem. 2003 Jan 2;46(1):49-63. doi: 10.1021/jm020241c. J Med Chem. 2003. PMID: 12502359
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.
Berger D, Dutia M, Powell D, Wu B, Wissner A, Boschelli DH, Floyd MB, Zhang N, Torres N, Levin J, Du X, Wojciechowicz D, Discafani C, Kohler C, Kim SC, Feldberg LR, Collins K, Mallon R. Berger D, et al. Among authors: floyd mb. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3031-4. doi: 10.1016/s0960-894x(03)00640-1. Bioorg Med Chem Lett. 2003. PMID: 12941327
2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.
Wissner A, Floyd MB, Johnson BD, Fraser H, Ingalls C, Nittoli T, Dushin RG, Discafani C, Nilakantan R, Marini J, Ravi M, Cheung K, Tan X, Musto S, Annable T, Siegel MM, Loganzo F. Wissner A, et al. Among authors: floyd mb. J Med Chem. 2005 Dec 1;48(24):7560-81. doi: 10.1021/jm050559f. J Med Chem. 2005. PMID: 16302797
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Wissner A, Fraser HL, Ingalls CL, Dushin RG, Floyd MB, Cheung K, Nittoli T, Ravi MR, Tan X, Loganzo F. Wissner A, et al. Among authors: floyd mb. Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. doi: 10.1016/j.bmc.2007.03.055. Epub 2007 Mar 23. Bioorg Med Chem. 2007. PMID: 17416531
Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785).
Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z, Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R, Shen R, Wang YF, Wissner A, Greenberger LM. Discafani CM, et al. Among authors: floyd mb jr. Biochem Pharmacol. 1999 Apr 15;57(8):917-25. doi: 10.1016/s0006-2952(98)00356-6. Biochem Pharmacol. 1999. PMID: 10086326
4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.
Wissner A, Berger DM, Boschelli DH, Floyd MB Jr, Greenberger LM, Gruber BC, Johnson BD, Mamuya N, Nilakantan R, Reich MF, Shen R, Tsou HR, Upeslacis E, Wang YF, Wu B, Ye F, Zhang N. Wissner A, et al. Among authors: floyd mb jr. J Med Chem. 2000 Aug 24;43(17):3244-56. doi: 10.1021/jm000206a. J Med Chem. 2000. PMID: 10966743
Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.
Kim KH, Wissner A, Floyd MB Jr, Fraser HL, Wang YD, Dushin RG, Hu Y, Olland A, Guo B, Arndt K. Kim KH, et al. Among authors: floyd mb jr. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5225-8. doi: 10.1016/j.bmcl.2009.07.007. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19628388
21 results