Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E, 4E)-5-arylpenta-2, 4-dienoic acid hydroxyamides

CM Marson, N Serradji, AS Rioja, SP Gastaud…

文献索引：Marson, Charles M.; Serradji, Nawal; Rioja, Alphonso S.; Gastaud, Sebastien P.; Alao, John P.; Coombes, R. Charles; Vigushin, David M. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2477 - 2481

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被引用次数: 19

摘要

Syntheses of (2E, 4E)-5-arylpenta-2, 4-dienoic acid hydroxyamides are described, some of which are potent inhibitors of histone deacetylase, a double bond conferring more than a 10- fold increase in potency compared with the triple bond analogue oxamflatin. Variation of substituents on the aromatic ring has a marked effect on potency, in vitro IC50 values down to 50nM being obtained.