title: Spin-labelled photo-cytotoxic diazido platinum(iv) anticancer complex.
abstract: We report the synthesis and characterisation of the nitroxide spin-labelled photoactivatable Pt(iv) prodrug trans,trans,trans-[Pt(N3)2(OH)(OCOCH2CH2CONH-TEMPO)(Py)2] (Pt-TEMPO, where TEMPO = 2,2,6,6-tetramethylpiperidine 1-oxyl). Irradiation with blue visible light gave rise to Pt(ii) and azidyl as well as nitroxyl radicals. Pt-TEMPO exhibited low toxicity in the dark, but on photoactivation was as active towards human ovarian cancer cells as the clinical photosensitizer chlorpromazine and much more active than the anticancer drug cisplatin under the conditions used.
authors.affiliation: Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK. P.J.Sadler@warwick.ac.uk.
authors.forename: V
authors.initials: V
authors.lastname: Venkatesh
authors.affiliation: Department of Physics, University of Warwick, Coventry CV4 7AL, UK. c.wedge@warwick.ac.uk.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Wedge
authors.affiliation: Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK. P.J.Sadler@warwick.ac.uk.
authors.forename: Isolda
authors.initials: I
authors.lastname: Romero-Canelón
authors.affiliation: Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK. P.J.Sadler@warwick.ac.uk.
authors.forename: Abraha
authors.initials: A
authors.lastname: Habtemariam
authors.affiliation: Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK. P.J.Sadler@warwick.ac.uk.
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Sadler
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003497:Cyclic N-Oxides / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008027:Light; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology; D013113:Spin Labels
chemical_list: D000970:Antineoplastic Agents; D003497:Cyclic N-Oxides; D011355:Prodrugs; D013113:Spin Labels; D010984:Platinum; C003959:TEMPO