title: 6,6″-Dimethyl-2,2':6',2″-terpyridine revisited: new fluorescent silver(I) helicates with in vitro antiproliferative activity via selective nucleoli targeting.
abstract: 6,6″-Dimethyl-2,2':6',2″-terpyridine ligand (L) reacts in equimolar ratio with Ag(I) ions what results in formation of dinuclear double helicates, which differ in terms of framework and complexity in accordance to counterions and solvent applied. Obtained complexes were thoroughly studied in terms of their biological activity, with the positive antiproliferative outcome on three human cancer cell lines: human breast cancer (T47D), human cervical carcinoma (HeLa) and human lung cancer (A-549). Performed DNA binding experiments showed that given Ag(I) species specifically interact with DNA double helix via intercalation and were visualized by confocal microscopy to specifically bind to the nuclei. All newly synthesized helical systems exhibit promising antimicrobial activity against Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus bacterial strains. Spectrophotometric properties were described as fulfilment of structural studies of newly presented complexes confirming their helical structure in solution.
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61614 Poznań, Poland.
authors.forename: Marta A
authors.initials: MA
authors.lastname: Fik
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61614 Poznań, Poland.
authors.forename: Adam
authors.initials: A
authors.lastname: Gorczyński
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61614 Poznań, Poland.
authors.forename: Maciej
authors.initials: M
authors.lastname: Kubicki
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61614 Poznań, Poland.
authors.forename: Zbigniew
authors.initials: Z
authors.lastname: Hnatejko
authors.affiliation: Institute of Bioorganic Chemistry, Polish Academy of Science, Noskowskiego 12/14, 61704 Poznań, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Fedoruk-Wyszomirska
authors.affiliation: Institute of Bioorganic Chemistry, Polish Academy of Science, Noskowskiego 12/14, 61704 Poznań, Poland.
authors.forename: Eliza
authors.initials: E
authors.lastname: Wyszko
authors.affiliation: Institute of Bioorganic Chemistry, Polish Academy of Science, Noskowskiego 12/14, 61704 Poznań, Poland.
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Giel-Pietraszuk
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61614 Poznań, Poland. Electronic address: violapat@amu.edu.pl.
authors.forename: Violetta
authors.initials: V
authors.lastname: Patroniak
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002466:Cell Nucleolus / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects*; D005453:Fluorescence; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012834:Silver / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: C000598938:6,6''-dimethyl-2,2':6',2''-terpyridine; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D011725:Pyridines; D012834:Silver
keywords: Antibacterial activity; Confocal microscopy; Cytotoxicity; Silver(I) helical complex; Spectroscopic DNA binding experiments; Terpyridine