title: Monofunctional platinum complexes containing a 4-nitrobenzo-2-oxa-1,3-diazole fluorophore: distribution in tumour cells.
abstract: Two monofunctional platinum(II) complexes, cis-[PtL(NH(3))(2)Cl]NO(3) (1) and cis-[PtL'(NH(3))(2)Cl]NO(3) (2) {L = N-methyl-7-nitro-N-(2-(pyridin-2-yl)ethyl)benzo[c][1,2,5]-oxadiazol-4-amine, L' = 7-nitro-N-(2-(pyridin-2-yl)ethyl)benzo[c][1,2,5] oxadiazol-4-amine}, have been synthesized and characterized. The X-ray single crystal structure of complex 1 shows that platinum(II) is coordinated in a square-planar geometry with a [PtN(3)Cl] setting. Fluorescence profiles of the complexes show that complex 1 is more suitable for cellular imaging than complex 2. The cellular uptake and distribution of complex 1 in the human cervical cancer HeLa cells were studied using confocal microscopy. Complex 1 enters the cells slowly, induces cytoplasmic vacuolations, and accumulates in the nucleoli. These results suggest that monofunctional platinum(II) complexes can stimulate tumour cells to undergo a nonapoptotic death process, which is distinct from the apoptosis induced by cisplatin.
authors.affiliation: State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, P.R. China.
authors.forename: Shengde
authors.initials: S
authors.lastname: Wu
authors.forename: Xiaoyong
authors.initials: X
authors.lastname: Wang
authors.forename: Chengcheng
authors.initials: C
authors.lastname: Zhu
authors.forename: Yajie
authors.initials: Y
authors.lastname: Song
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.forename: Yizhi
authors.initials: Y
authors.lastname: Li
authors.forename: Zijian
authors.initials: Z
authors.lastname: Guo
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000737:chemistry* / Q000493:pharmacokinetics; D018360:Crystallography, X-Ray; D006801:Humans; D007536:Isomerism; D018613:Microscopy, Confocal; D008968:Molecular Conformation; D009369:Neoplasms / Q000188:drug therapy; D010069:Oxadiazoles / Q000737:chemistry*; D010984:Platinum / Q000737:chemistry*; D013050:Spectrometry, Fluorescence
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010069:Oxadiazoles; C011514:4-nitrobenzofurazan; D010984:Platinum