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Page 1
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: discafani c. J Med Chem. 2005 Dec 1;48(24):7560-81. doi: 10.1021/jm050559f. J Med Chem. 2005. PMID: 16302797
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: discafani c. J Med Chem. 2003 Jan 2;46(1):49-63. doi: 10.1021/jm020241c. J Med Chem. 2003. PMID: 12502359
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: discafani c. J Med Chem. 2005 Feb 24;48(4):1107-31. doi: 10.1021/jm040159c. J Med Chem. 2005. PMID: 15715478
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
Tsou HR, Mamuya N, Johnson BD, Reich MF, Gruber BC, Ye F, Nilakantan R, Shen R, Discafani C, DeBlanc R, Davis R, Koehn FE, Greenberger LM, Wang YF, Wissner A. Tsou HR, et al. Among authors: discafani c. J Med Chem. 2001 Aug 16;44(17):2719-34. doi: 10.1021/jm0005555. J Med Chem. 2001. PMID: 11495584
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: discafani c. 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
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, Annable T, Yang X, Discafani C, Beyer C, Greenberger LM, Loganzo F, Ayral-Kaloustian S. Zask A, et al. Among authors: discafani c. J Med Chem. 2004 Sep 9;47(19):4774-86. doi: 10.1021/jm040056u. J Med Chem. 2004. PMID: 15341492
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. Biochem Pharmacol. 1999 Apr 15;57(8):917-25. doi: 10.1016/s0006-2952(98)00356-6. Biochem Pharmacol. 1999. PMID: 10086326
27 results