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Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrrolidin-1-yl)-ethoxy]-phenyl}-amine).
Hu SX, Soll R, Yee S, Lohse DL, Kousba A, Zeng B, Yu X, McPherson A, Renick J, Cao J, Tabak A, Hood J, Doukas J, Noronha G, Martin M. Hu SX, et al. Among authors: mcpherson a. Drug Metab Dispos. 2007 Jun;35(6):929-36. doi: 10.1124/dmd.106.014290. Epub 2007 Mar 19. Drug Metab Dispos. 2007. PMID: 17371799
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Noronha G, Barrett K, Boccia A, Brodhag T, Cao J, Chow CP, Dneprovskaia E, Doukas J, Fine R, Gong X, Gritzen C, Gu H, Hanna E, Hood JD, Hu S, Kang X, Key J, Klebansky B, Kousba A, Li G, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Shi F, Soll R, Splittgerber U, Stoughton S, Tang S, Yee S, Zeng B, Zhao N, Zhu H. Noronha G, et al. Among authors: mcpherson a. Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. doi: 10.1016/j.bmcl.2006.11.006. Epub 2006 Nov 7. Bioorg Med Chem Lett. 2007. PMID: 17113292
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.
Palanki MS, Akiyama H, Campochiaro P, Cao J, Chow CP, Dellamary L, Doukas J, Fine R, Gritzen C, Hood JD, Hu S, Kachi S, Kang X, Klebansky B, Kousba A, Lohse D, Mak CC, Martin M, McPherson A, Pathak VP, Renick J, Soll R, Umeda N, Yee S, Yokoi K, Zeng B, Zhu H, Noronha G. Palanki MS, et al. Among authors: mcpherson a. J Med Chem. 2008 Mar 27;51(6):1546-59. doi: 10.1021/jm7011276. Epub 2008 Feb 27. J Med Chem. 2008. PMID: 18311895
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Noronha G, Barrett K, Cao J, Dneprovskaia E, Fine R, Gong X, Gritzen C, Hood J, Kang X, Klebansky B, Li G, Liao W, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Soll R, Splittgerber U, Wrasidlo W, Zeng B, Zhao N, Zhou Y. Noronha G, et al. Among authors: mcpherson a. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5546-50. doi: 10.1016/j.bmcl.2006.08.035. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931012
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Cao J, Fine R, Gritzen C, Hood J, Kang X, Klebansky B, Lohse D, Mak CC, McPherson A, Noronha G, Palanki MS, Pathak VP, Renick J, Soll R, Zeng B, Zhu H. Cao J, et al. Among authors: mcpherson a. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5812-8. doi: 10.1016/j.bmcl.2007.08.043. Epub 2007 Aug 25. Bioorg Med Chem Lett. 2007. PMID: 17827012
Development of novel benzotriazines for drug discovery.
Palanki MS, Cao J, Chow CP, Dneprovskaia E, Mak CC, McPherson A, Pathak VP, Renick J, Soll R, Zeng B, Noronha G. Palanki MS, et al. Among authors: mcpherson a. Expert Opin Drug Discov. 2009 Jan;4(1):33-49. doi: 10.1517/17460440802580536. Epub 2008 Dec 10. Expert Opin Drug Discov. 2009. PMID: 23480335
752 results