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  • Title: Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.
    Author: Mesaros EF, Angeles TS, Albom MS, Wagner JC, Aimone LD, Wan W, Lu L, Huang Z, Olsen M, Kordwitz E, Haltiwanger RC, Landis AJ, Cheng M, Ruggeri BA, Ator MA, Dorsey BD, Ott GR.
    Journal: Bioorg Med Chem Lett; 2015 Mar 01; 25(5):1047-52. PubMed ID: 25655723.
    Abstract:
    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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