title: Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
abstract: 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 IC(50) values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC(50) of approximately 1.5 microM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical trials.
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, London WC1H OAJ, UK. c.m.marson@ucl.ac.uk
authors.forename: Charles M
authors.initials: CM
authors.lastname: Marson
authors.forename: Pascal
authors.initials: P
authors.lastname: Savy
authors.forename: Alphonso S
authors.initials: AS
authors.lastname: Rioja
authors.forename: Thevaki
authors.initials: T
authors.lastname: Mahadevan
authors.forename: Catherine
authors.initials: C
authors.lastname: Mikol
authors.forename: Arthi
authors.initials: A
authors.lastname: Veerupillai
authors.forename: Eva
authors.initials: E
authors.lastname: Nsubuga
authors.forename: Angela
authors.initials: A
authors.lastname: Chahwan
authors.forename: Simon P
authors.initials: SP
authors.lastname: Joel
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D013011:Sorbic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis* / Q000494:pharmacology; D013441:Sulfinic Acids / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D013440:Sulfides; D013441:Sulfinic Acids; D013011:Sorbic Acid