title: 5-membered cyclic hydroxamic acids as HDAC inhibitors.
abstract: The new histone deacylases inhibitors (HDACi) were synthesized in the class of 5-membered cyclic hydroxamic acids (5-CHA), showing medium size CHA as a new Zn-binding group. New reaction sequence was proposed for the synthesis of 5-membered alkylidene-cyclic-hydroxamic acids starting from butyrolactone. Compound 10c showed low µM activity on HeLa cell extracts. From these results, cyclic hydroxamic acids will be further investigated to find more potent compounds.
authors.affiliation: Department of Organic Chemistry, Latvian Institute of Organic Synthesis , Riga , Latvia.
authors.forename: Ilze
authors.initials: I
authors.lastname: Mutule
authors.forename: Diana
authors.initials: D
authors.lastname: Borovika
authors.forename: Elina
authors.initials: E
authors.lastname: Rozenberga
authors.forename: Nadezhda
authors.initials: N
authors.lastname: Romanchikova
authors.forename: Raivis
authors.initials: R
authors.lastname: Zalubovskis
authors.forename: Irina
authors.initials: I
authors.lastname: Shestakova
authors.forename: Peteris
authors.initials: P
authors.lastname: Trapencieris
mesh_terms: D000147:Acids, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006367:HeLa Cells; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000147:Acids, Heterocyclic; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids
keywords: Cyclic hydroxamic acids; N-hydroxypyrrolidones; histone deacylases; inhibitors