title: Naphthalimide gold(I) phosphine complexes as anticancer metallodrugs.
abstract: Gold(I) phosphine complexes exhibit promising properties for anticancer drug development. Here we report on a series of gold(I) phosphine complexes containing a naphthalimide ligand. Strong antiproliferative effects were observed in MCF-7 breast cancer cells as well as in HT-29 colon carcinoma cells. The cellular and nuclear gold levels were increased compared to analogues, in which the naphthalimide ligand was replaced by a chloro ligand. Compound 4a was selected for more detailed biochemical and biological studies, which revealed solvent dependent fluorescence emission, uptake of the compound into the organelles of tumor cells as well as antiangiogenic effects concerning angiogenesis and tumor-induced angiogenesis in vivo. Antiangiogenic properties of 4a were observed in two different zebrafish angiogenesis models, including a tumor-cell induced neovascularization assay.
authors.affiliation: Department of Integrative Zoology, Institute of Biology, University of Leiden, 2333 AL Leiden, The Netherlands.
authors.forename: Christoph P
authors.initials: CP
authors.lastname: Bagowski
authors.forename: Ya
authors.initials: Y
authors.lastname: You
authors.forename: Heike
authors.initials: H
authors.lastname: Scheffler
authors.forename: Danielle H
authors.initials: DH
authors.lastname: Vlecken
authors.forename: Daan J
authors.initials: DJ
authors.lastname: Schmitz
authors.forename: Ingo
authors.initials: I
authors.lastname: Ott
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D047108:Embryonic Development / Q000187:drug effects; D006046:Gold / Q000737:chemistry*; D019073:HT29 Cells; D006801:Humans; D053644:Naphthalimides / Q000737:chemistry*; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010720:Phosphines / Q000737:chemistry*; D013050:Spectrometry, Fluorescence; D015027:Zebrafish
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D053644:Naphthalimides; D009942:Organometallic Compounds; D010720:Phosphines; D006046:Gold; C044646:phosphine