Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

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Bergman JM, Abrams MT, Davide JP, Greenberg IB, Robinson RG, Buser CA, Huber HE, Koblan KS, Kohl NE, Lobell RB, Graham SL, Hartman GD, Williams TM, Dinsmore CJ

Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1411-5.

PubMed ID

11378366 [ View in PubMed

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Abstract

A series of aryloxy substituted piperazinones with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to have potent inhibitory activity in vitro and are promising agents for the inhibition of Ki-Ras signaling.

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
L-778123	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	IC 50 (nM)	98000	N/A	N/A	Details
L-778123	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	IC 50 (nM)	3	N/A	N/A	Details