title: Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation.
abstract: Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies and preliminary biological evaluation give insights into their mechanism of action and the potential of this strategy.
authors.affiliation: Department of Chemistry, University of Liverpool, Crown Street, Liverpool L69 7ZD, UK.
authors.forename: Louise
authors.initials: L
authors.lastname: La Pensée
authors.forename: Sunil
authors.initials: S
authors.lastname: Sabbani
authors.forename: Raman
authors.initials: R
authors.lastname: Sharma
authors.forename: Inder
authors.initials: I
authors.lastname: Bhamra
authors.forename: Emma
authors.initials: E
authors.lastname: Shore
authors.forename: Amy E
authors.initials: AE
authors.lastname: Chadwick
authors.forename: Neil G
authors.initials: NG
authors.lastname: Berry
authors.forename: James
authors.initials: J
authors.lastname: Firman
authors.forename: Nuna C
authors.initials: NC
authors.lastname: Araujo
authors.forename: Lília
authors.initials: L
authors.lastname: Cabral
authors.forename: Maria L S
authors.initials: ML
authors.lastname: Cristiano
authors.forename: Cerys
authors.initials: C
authors.lastname: Bateman
authors.forename: Omar
authors.initials: O
authors.lastname: Janneh
authors.forename: Adelina
authors.initials: A
authors.lastname: Gavrila
authors.forename: Yi Hang
authors.initials: YH
authors.lastname: Wu
authors.forename: Afthab
authors.initials: A
authors.lastname: Hussain
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Ward
authors.forename: Paul A
authors.initials: PA
authors.lastname: Stocks
authors.forename: Rick
authors.initials: R
authors.lastname: Cosstick
authors.forename: Paul M
authors.initials: PM
authors.lastname: O'Neill
mesh_terms: D000971:Antineoplastic Combined Chemotherapy Protocols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D019073:HT29 Cells; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D056004:Molecular Dynamics Simulation; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011108:Polymers / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013816:Thermodynamics
chemical_list: D037621:Artemisinins; D011108:Polymers; D011758:Pyrroles; C067635:polypyrrole; D004247:DNA; C031327:artemisinin