title: Tyrosyl-DNA Phosphodiesterase I Inhibitors from the Australian Plant Macropteranthes leichhardtii.
abstract: Mass-directed isolation of the CH2Cl2/MeOH extract from the bark of an Australian plant, Macropteranthes leichhardtii, resulted in the purification of a new phenylpropanoid glucoside, macropteranthol (1), together with four known analogues (2-5). The structure of compound 1 was elucidated by NMR and MS data analyses and quantum chemical calculations. Compounds 3 and 5 showed inhibitory activity against tyrosyl-DNA phosphodiesterase I with IC50 values of ∼1.0 μM.
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Li-Wen
authors.initials: LW
authors.lastname: Tian
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Yunjiang
authors.initials: Y
authors.lastname: Feng
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Trong D
authors.initials: TD
authors.lastname: Tran
authors.affiliation: ‡Centre for Drug Research and Development, Vancouver, BC 2405, Canada.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Shimizu
authors.affiliation: ‡Centre for Drug Research and Development, Vancouver, BC 2405, Canada.
authors.forename: Tom
authors.initials: T
authors.lastname: Pfeifer
authors.affiliation: §Queensland Herbarium, Toowong, QLD 4066, Australia.
authors.forename: Paul I
authors.initials: PI
authors.lastname: Forster
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Quinn
mesh_terms: D001315:Australia; D029764:Combretaceae / Q000737:chemistry*; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010666:Phenylpropionates / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D005960:Glucosides; D010666:Phenylpropionates; D010726:Phosphodiesterase Inhibitors; C000602070:macropteranthol; D010727:Phosphoric Diester Hydrolases; C122147:tyrosyl-DNA phosphodiesterase