title: Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
abstract: delta-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology, Yuseong, Daejeon 305-333, Republic of Korea.
authors.forename: Hwan Mook
authors.initials: HM
authors.lastname: Kim
authors.forename: Kiho
authors.initials: K
authors.lastname: Lee
authors.forename: Bum Woo
authors.initials: BW
authors.lastname: Park
authors.forename: Dong Kyu
authors.initials: DK
authors.lastname: Ryu
authors.forename: Kangjeon
authors.initials: K
authors.lastname: Kim
authors.forename: Chang Woo
authors.initials: CW
authors.lastname: Lee
authors.forename: Song-Kyu
authors.initials: SK
authors.lastname: Park
authors.forename: Jung Whan
authors.initials: JW
authors.lastname: Han
authors.forename: Hee Yoon
authors.initials: HY
authors.lastname: Lee
authors.forename: Hyun Yong
authors.initials: HY
authors.lastname: Lee
authors.forename: Gyoonhee
authors.initials: G
authors.lastname: Han
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors