title: Inhibition of topoisomerase I by naphthoquinone derivatives.
abstract: Alkannin and shikonin are naturally occurring naphthoquinones. We have tested several derivatives of the title compounds and we have found that naphthoquinones bearing at least one phenolic hydroxyl group are potent inhibitors of topoisomerase I. The ability of the tested compounds to complex Zn++ parallels with a few exceptions their topoisomerase I inhibition properties while their intercalation and redox properties do not.
authors.affiliation: Chemistry Laboratories, Agricultural University of Athens, Greece.
authors.forename: Z F
authors.initials: ZF
authors.lastname: Plyta
authors.forename: T
authors.initials: T
authors.lastname: Li
authors.forename: V P
authors.initials: VP
authors.lastname: Papageorgiou
authors.forename: A S
authors.initials: AS
authors.lastname: Mellidis
authors.forename: A N
authors.initials: AN
authors.lastname: Assimopoulou
authors.forename: E N
authors.initials: EN
authors.lastname: Pitsinos
authors.forename: E A
authors.initials: EA
authors.lastname: Couladouros
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology*; D009285:Naphthoquinones / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors; D015032:Zinc / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D009285:Naphthoquinones; D059004:Topoisomerase I Inhibitors; D015032:Zinc