title: Histone deacetylase inhibitors derived from  1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related  heterocycles selective for the HDAC6 isoform.
abstract: Acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide are potent sub-type selective HDAC6 inhibitors. Constrained heterocyclic analogs based on 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine show further enhanced HDAC6 selectivity and inhibitory activity in cells. Homology models suggest that the heterocyclic spacer can more effectively access the wider catalytic channel of HDAC6 compared to other HDAC sub-types.
authors.forename: Christopher
authors.initials: C
authors.lastname: Blackburn
authors.forename: Cynthia
authors.initials: C
authors.lastname: Barrett
authors.forename: Mable
authors.initials: M
authors.lastname: Brunson
authors.forename: Janice
authors.initials: J
authors.lastname: Chin
authors.forename: Dylan
authors.initials: D
authors.lastname: England
authors.forename: Kris
authors.initials: K
authors.lastname: Garcia
authors.forename: Kenneth
authors.initials: K
authors.lastname: Gigstad
authors.forename: Alexandra
authors.initials: A
authors.lastname: Gould
authors.forename: Juan
authors.initials: J
authors.lastname: Gutierrez
authors.forename: Kara
authors.initials: K
authors.lastname: Hoar
authors.forename: R Scott
authors.initials: RS
authors.lastname: Rowland
authors.forename: Christopher
authors.initials: C
authors.lastname: Tsu
authors.forename: John
authors.initials: J
authors.lastname: Ringeling
authors.forename: Krista
authors.initials: K
authors.lastname: Wager
authors.forename: He
authors.initials: H
authors.lastname: Xu
mesh_terms: D056572:Histone Deacetylase Inhibitors / Q000378:metabolism*; D006877:Hydroxamic Acids / Q000494:pharmacology*; D020033:Protein Isoforms; D011719:Pyrazines / Q000378:metabolism*
chemical_list: D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D020033:Protein Isoforms; D011719:Pyrazines