Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors

Mercaptoacetamides were designed and synthesized as HDAC inhibitors. A series of mercaptoacetamides were designed and synthesized as novel histone deacetylase inhibitors with the aid of modeling. Their ability to inhibit HDAC activity and their effects on cancer cell growth were investigated. Some c...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (5), p.1389-1392
Main Authors: Chen, Bin, Petukhov, Pavel A., Jung, Mira, Velena, Alfredo, Eliseeva, Elena, Dritschilo, Anatoly, Kozikowski, Alan P.
Format: Article
Language:English
Subjects:
Acetamides - chemistry
Acetamides - pharmacology
Antineoplastic agents
Binding Sites
Biological and medical sciences
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
HDAC
Histone deacetylase inhibitor
Histone Deacetylase Inhibitors
Medical sciences
Mercaptoacetamide
Models, Molecular
Molecular Conformation
Pharmacology. Drug treatments
Structure-Activity Relationship
Sulfhydryl Compounds - chemistry
Sulfhydryl Compounds - pharmacology
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Summary:Mercaptoacetamides were designed and synthesized as HDAC inhibitors. A series of mercaptoacetamides were designed and synthesized as novel histone deacetylase inhibitors with the aid of modeling. Their ability to inhibit HDAC activity and their effects on cancer cell growth were investigated. Some compounds exhibit better HDAC inhibitory activity than SAHA.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.01.006