Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors

Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal microsomal reactive metabolite formation were dis...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-01, Vol.55 (1), p.115-125
Hauptverfasser:	Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Aniline Compounds - chemical synthesis Aniline Compounds - pharmacokinetics Aniline Compounds - pharmacology Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Biological Availability In Vitro Techniques Mice Mice, SCID Microsomes, Liver - metabolism Pyrroles - chemical synthesis Pyrroles - pharmacokinetics Pyrroles - pharmacology Rats Rats, Sprague-Dawley Receptor Protein-Tyrosine Kinases - antagonists & inhibitors Structure-Activity Relationship Triazines - chemical synthesis Triazines - pharmacokinetics Triazines - pharmacology Xenograft Model Antitumor Assays
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