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Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors
- Source :
- Journal of medicinal chemistry. 46(5)
- Publication Year :
- 2003
-
Abstract
- A series of sulfonamide hydroxamic acids and anilides have been synthesized and studied as histone deacetylase (HDAC) inhibitors that can induce hyperacetylation of histones in human cancer cells. The inhibition of HDAC activity represents a novel approach for intervening in cell cycle regulation. The lead candidates were screened in a panel of human tumor and normal cell lines. They selectively inhibit proliferation, cause cell cycle blocks, and induce apoptosis in human cancer cells but not in normal cells. The structure-activity relationships, the antiproliferative activity, and the in vivo efficacy are described.
- Subjects :
- Transplantation, Heterologous
Mice, Nude
Antineoplastic Agents
Hydroxamic Acids
Cell Line
chemistry.chemical_compound
Mice
Structure-Activity Relationship
Drug Discovery
Animals
Humans
Enzyme Inhibitors
Histone deacetylase 5
Sulfonamides
Hydroxamic acid
biology
HDAC11
Histone deacetylase 2
Cell Cycle
Histone acetyltransferase
Cell cycle
Histone Deacetylase Inhibitors
Histone
chemistry
Biochemistry
Cancer research
biology.protein
Molecular Medicine
Histone deacetylase
Drug Screening Assays, Antitumor
Neoplasm Transplantation
Subjects
Details
- ISSN :
- 00222623
- Volume :
- 46
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....bf49c65361da45cf1ea542acf1aa99e0