Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

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Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43.

PubMed ID

14741259 [ View in PubMed

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Abstract

A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed.

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)	2	N/A	N/A	Details
L-778123	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	IC 50 (nM)	98	N/A	N/A	Details
L-778123	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	IC 50 (nM)	3.6	N/A	N/A	Details