Abstract
A novel series of non-hydroxamate HDAC inhibitors (HDACi) showing a uracil group at the left and a 2-aminoanilide/2-aminoanilide-like portion at the right head have been reported. In particular, the new compounds incorporating a 2-aminoanilide moiety behaved as class I-selective HDACi. Compound 8, the most potent and class I-selective, showed weak apoptosis (higher than MS-275) joined to cytodifferentiating activity on U937 cells. Surprisingly, the highest differentiation was observed with 13, through an effect that seems to be unrelated to HDAC inhibition.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylation
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Amination
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Benzamidines / chemical synthesis*
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Benzamidines / chemistry
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Benzamidines / pharmacology*
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Cell Differentiation / drug effects
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Granulocytes / cytology
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Granulocytes / drug effects
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Histone Deacetylase Inhibitors*
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Histone Deacetylases / metabolism
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Histones / metabolism
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Humans
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Molecular Structure
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
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U937 Cells
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Uracil / chemistry
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Uracil / pharmacology*
Substances
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Benzamidines
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Histone Deacetylase Inhibitors
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Histones
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Recombinant Proteins
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Uracil
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Histone Deacetylases