Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

Basic Information

ID: ALA1134196

Journal: Bioorg Med Chem Lett

Title: Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

Authors: Dinsmore CJ, Bergman JM, Wei DD, Zartman CB, Davide JP, Greenberg IB, Liu D, O'Neill TJ, Gibbs JB, Koblan KS, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM.

Abstract: The evaluation of SAR associated with the insertion of carbonyl groups at various positions of N-arylpiperazinone farnesyltransferase inhibitors is described herein. 1-Aryl-2,3-diketopiperazine derivatives exhibited the best balance of potency and pharmacokinetic profile relative to the parent 1-aryl-2-piperazinones.

CiteXplore: 11229765

DOI: 10.1016/s0960-894x(00)00710-1

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