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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.

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.
J Med Chem; 55(1): 115-25, 2012 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-22141319
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 discovered. Potent, selective, and metabolically stable ALK inhibitors from this class were identified, and an orally bioavailable compound (32) with antitumor efficacy in ALK-driven xenografts in mouse models was extensively characterized.
Selo DaSilva