title: Polyfluorinated bipyridine cisplatins manipulate cytotoxicity through the induction of S-G2/M arrest and partial intercalation mechanism.
abstract: A series of polyfluorinated bipyridine cisplatins 2-6 were prepared, characterized, and evaluated for their in vitro cytotoxicities against a panel of human cancer cell lines, MCF7 (breast adenocarcinoma), MDA-MB-231 (breast adenocarcinoma) and A549 (lung adenocarcinoma). The results show that a correlation between the relative order of lipophilicity of complexes 2-4 and their cytotoxicity is established by following the trend: 4>2>3. Complex 4, which is the most active compound in the series, was found to be a more effective and selective anticancer agent than cisplatin. Complex 4 inhibited cancer cell proliferation by partial intercalation to DNA, which subsequently resulted in induction of S-G2/M arrest and apoptosis.
authors.affiliation: Institute of Chemistry, Academia Sinica, Taipei 115, Taiwan.
authors.forename: Tzu Ting
authors.initials: TT
authors.lastname: Chang
authors.forename: Shivaji V
authors.initials: SV
authors.lastname: More
authors.forename: Norman
authors.initials: N
authors.lastname: Lu
authors.forename: Jyun-Wei
authors.initials: JW
authors.lastname: Jhuo
authors.forename: Yi-Chuan
authors.initials: YC
authors.lastname: Chen
authors.forename: Shu-Chuan
authors.initials: SC
authors.lastname: Jao
authors.forename: Wen-Shan
authors.initials: WS
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002453:Cell Cycle / Q000187:drug effects*; D002945:Cisplatin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D054879:Halogenation; D006801:Humans; D007364:Intercalating Agents / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D015394:Molecular Structure; D011725:Pyridines / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D059807:S Phase Cell Cycle Checkpoints / Q000187:drug effects; D012984:Software; D014407:Tumor Cells, Cultured / Q000166:cytology
chemical_list: D000970:Antineoplastic Agents; D007364:Intercalating Agents; D011725:Pyridines; D002945:Cisplatin