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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

Mesaros, Eugen F; Angeles, Thelma S; Albom, Mark S; Wagner, Jason C; Aimone, Lisa D; Wan, Weihua; Lu, Lihui; Huang, Zeqi; Olsen, Mark; Kordwitz, Emily; Haltiwanger, R Curtis; Landis, Amy J; Cheng, Mangeng; Ruggeri, Bruce A; Ator, Mark A; Dorsey, Bruce D; Ott, Gregory R.
Bioorg Med Chem Lett; 25(5): 1047-52, 2015 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-25655723
The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of anaplastic lymphoma kinase (ALK) are described. Although piperidine-3,4-diol and piperidine-3-ol derivatives showed comparable in vitro ALK activity, the latter subset of inhibitors demonstrated improved physiochemical and pharmacokinetic properties. Furthermore, the stereochemistry of the C3 and C4 centers had a marked impact on the in vivo inhibition of ALK autophosphorylation. Thus, trans-4-aryl-piperidine-3-ols (22) were more potent than the cis diastereomers (20).
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