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

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

  • Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81. doi: 10.1016/j.bmcl.2004.03.012.
Charles M Marson 1,  Nawal Serradji,  Alphonso S Rioja,  Sebastien P Gastaud,  John P Alao,  R Charles Coombes,  David M Vigushin
Affiliations

Affiliation

  • 1 Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK. [email protected]
PMID: 15109636 DOI: 10.1016/j.bmcl.2004.03.012
Abstract

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 IC(50) values down to 50 nM being obtained.

Figures