title: Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.
abstract: We have designed and synthesized a series of structurally novel hydroxamic acid-based histone deacetylase (HDAC) inhibitors characterized by a zinc chelating head group attached directly to a thiazole ring. The thiazole ring connects to a piperazine spacer, which is capped with a sulfonamide group. These novel molecules potently inhibit an HDAC enzyme mixture derived from HeLa cervical carcinoma cells and show potent antiproliferative activity against the breast cancer cell line MCF7.
authors.affiliation: EntreMed Inc., 101 College Street, Toronto Medical Discovery Tower, Toronto, Ontario, Canada M5G1L7. skumar@aretetherapeutics.com
authors.forename: Sampath-Kumar
authors.initials: SK
authors.lastname: Anandan
authors.forename: John S
authors.initials: JS
authors.lastname: Ward
authors.forename: Richard D
authors.initials: RD
authors.lastname: Brokx
authors.forename: Trisha
authors.initials: T
authors.lastname: Denny
authors.forename: Mark R
authors.initials: MR
authors.lastname: Bray
authors.forename: Dinesh V
authors.initials: DV
authors.lastname: Patel
authors.forename: Xiao-Yi
authors.initials: XY
authors.lastname: Xiao
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006367:HeLa Cells; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship