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Page 1
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: tsou hr. 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. J Med Chem. 2005 Feb 24;48(4):1107-31. doi: 10.1021/jm040159c. J Med Chem. 2005. PMID: 15715478
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
Wissner A, Brawner Floyd MB, Rabindran SK, Nilakantan R, Greenberger LM, Shen R, Wang YF, Tsou HR. Wissner A, et al. Among authors: tsou hr. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2893-7. doi: 10.1016/s0960-894x(02)00598-x. Bioorg Med Chem Lett. 2002. PMID: 12270171
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. J Med Chem. 2001 Aug 16;44(17):2719-34. doi: 10.1021/jm0005555. J Med Chem. 2001. PMID: 11495584
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: tsou hr. J Med Chem. 2000 Aug 24;43(17):3244-56. doi: 10.1021/jm000206a. J Med Chem. 2000. PMID: 10966743
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Tsou HR, Liu X, Birnberg G, Kaplan J, Otteng M, Tran T, Kutterer K, Tang Z, Suayan R, Zask A, Ravi M, Bretz A, Grillo M, McGinnis JP, Rabindran SK, Ayral-Kaloustian S, Mansour TS. Tsou HR, et al. J Med Chem. 2009 Apr 23;52(8):2289-310. doi: 10.1021/jm801026e. J Med Chem. 2009. PMID: 19317452
18 results