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

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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

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

Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.

PubMed ID

11229765 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
L-778123	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	IC 50 (nM)	2000	N/A	N/A	Details