Inhibitors of Human Histone Deacetylase:  Synthesis and Enzyme and Cellular Activity of Straight Chain Hydroxamates

Journal of Medicinal Chemistry
2002.0

Abstract

Inhibitors 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 p21(waf1) (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.

Knowledge Graph

Similar Paper

Inhibitors of Human Histone Deacetylase:  Synthesis and Enzyme and Cellular Activity of Straight Chain Hydroxamates
Journal of Medicinal Chemistry 2002.0
Biological and Biophysical Properties of the Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid Are Affected by the Presence of Short Alkyl Groups on the Phenyl Ring
Journal of Medicinal Chemistry 2010.0
Novel Inhibitors of Human Histone Deacetylases:  Design, Synthesis, Enzyme Inhibition, and Cancer Cell Growth Inhibition of SAHA-Based Non-hydroxamates
Journal of Medicinal Chemistry 2005.0
Structurally Simple Trichostatin A-Like Straight Chain Hydroxamates as Potent Histone Deacetylase Inhibitors
Journal of Medicinal Chemistry 2002.0
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2016.0
A New Simple and High-Yield Synthesis of Suberoylanilide Hydroxamic Acid and Its Inhibitory Effect Alone or in Combination with Retinoids on Proliferation of Human Prostate Cancer Cells
Journal of Medicinal Chemistry 2005.0
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-Based non-hydroxamates
Bioorganic & Medicinal Chemistry Letters 2003.0
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group
Bioorganic & Medicinal Chemistry Letters 2004.0
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
Bioorganic & Medicinal Chemistry Letters 2007.0
Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors
Bioorganic & Medicinal Chemistry 2014.0