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

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

Bioorganic & medicinal chemistry letters (2001-05-30)

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

PMID11378366

摘要

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.