jm015568c_si_002.pdf (88.15 kB)
Inhibitors of Human Histone Deacetylase: Synthesis and Enzyme and Cellular Activity of Straight Chain Hydroxamates
journal contribution
posted on 2002-01-17, 00:00 authored by Stacy W. Remiszewski, Lidia C. Sambucetti, Peter Atadja, Kenneth W. Bair, Wendy D. Cornell, Michael A. Green, Kobporn Lulu Howell, Manfred Jung, Paul Kwon, Nancy Trogani, Heather WalkerInhibitors of histone deacetylase (HDAC) have been
shown to induce terminal differentiation of human tumor cell
lines and to have antitumor effects in vivo. We have prepared
analogues of suberoylanilide hydroxamic acid (SAHA) and
trichostatin A and have evaluated them in a human HDAC
enzyme inhibition assay, a p21waf1 (p21) promoter assay, and
in monolayer growth inhibition assays. One compound, 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-benzamide, was
found to affect the growth of a panel of eight human tumor
cell lines differentially.