Abstract
Histone deacetylases (HDACs) are a promising target for treating cancer and some other disorders. Herein, based on the structure of our previously reported tetrahydroisoquinoline-based hydroxamic acids, a novel series of tyrosine-based hydroxamic acid derivatives was designed and synthesized as HDACs inhibitors. Compared with tetrahydroisoquinoline-based hydroxamic acids, tyrosine-based hydroxamic acid derivatives exhibited more potent HDAC8 inhibitory activity. However, the antiproliferative activities and HeLa cell nuclear extract inhibition of several selected tyrosine-based hydroxamic acids were moderate.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Cell Survival / drug effects
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Drug Design*
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HeLa Cells
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Histone Deacetylase Inhibitors / chemical synthesis
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Histone Deacetylase Inhibitors / chemistry*
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Histone Deacetylase Inhibitors / pharmacology*
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Histone Deacetylases / metabolism
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Humans
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Hydroxamic Acids / chemical synthesis
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Hydroxamic Acids / chemistry
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Hydroxamic Acids / pharmacology
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Neoplasms / drug therapy*
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Neoplasms / enzymology
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Repressor Proteins / antagonists & inhibitors*
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Repressor Proteins / metabolism
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Structure-Activity Relationship
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Tyrosine / chemical synthesis
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Tyrosine / chemistry
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Tyrosine / pharmacology
Substances
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Antineoplastic Agents
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Histone Deacetylase Inhibitors
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Hydroxamic Acids
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Repressor Proteins
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Tyrosine
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HDAC8 protein, human
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Histone Deacetylases