Aromatic Sulfide Inhibitors of Histone Deacetylase Based on Arylsulfinyl-2,4-hexadienoic Acid Hydroxyamides

The synthesis of a novel series of potent inhibitors of histone deacetylases is described, based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides and their derivatives. In vitro IC50 values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-01, Vol.49 (2), p.800-805
Hauptverfasser:	Marson, Charles M, Savy, Pascal, Rioja, Alphonso S, Mahadevan, Thevaki, Mikol, Catherine, Veerupillai, Arthi, Nsubuga, Eva, Chahwan, Angela, Joel, Simon P
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - pharmacology Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor Drug Screening Assays, Antitumor General aspects Histone Deacetylase Inhibitors Humans Medical sciences Pharmacology. Drug treatments Sorbic Acid - analogs & derivatives Sorbic Acid - chemical synthesis Sorbic Acid - pharmacology Structure-Activity Relationship Sulfides - chemical synthesis Sulfides - pharmacology Sulfinic Acids - chemical synthesis Sulfinic Acids - pharmacology
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Zusammenfassung:	The synthesis of a novel series of potent inhibitors of histone deacetylases is described, based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides and their derivatives. In vitro IC50 values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC50 of ∼1.5 μM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical trials.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm051010j