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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: dushin rg. 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
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: dushin rg. J Med Chem. 2005 Dec 1;48(24):7560-81. doi: 10.1021/jm050559f. J Med Chem. 2005. PMID: 16302797
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: dushin rg. 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
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).
Nittoli T, Dushin RG, Ingalls C, Cheung K, Floyd MB, Fraser H, Olland A, Hu Y, Grosu G, Han X, Arndt K, Guo B, Wissner A. Nittoli T, et al. Among authors: dushin rg. Eur J Med Chem. 2010 Apr;45(4):1379-86. doi: 10.1016/j.ejmech.2009.12.036. Epub 2009 Dec 28. Eur J Med Chem. 2010. PMID: 20074837
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.
Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI. Zapf CW, et al. Among authors: dushin rg. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4602-7. doi: 10.1016/j.bmcl.2011.05.102. Epub 2011 Jun 27. Bioorg Med Chem Lett. 2011. PMID: 21715165
38 results