Bioorganic & Medicinal Chemistry Letters 2001-06-04

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

J M Bergman, M T Abrams, J P Davide, I B Greenberg, R G Robinson, C A Buser, H E Huber, K S Koblan, N E Kohl, R B Lobell, S L Graham, G D Hartman, T M Williams, C J Dinsmore

Index: Bioorg. Med. Chem. Lett. 11(11) , 1411-5, (2001)

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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.