title: Platinum (II) complexes with stereochemically-defined thiepane dioxide diamine ligands as anticancer drugs.
abstract: Platinum (II) complexes are accredited with biological activities. New complexes with thiepane dioxide diamine as ligands, characterized by defined stereochemical features, a flexible 7-membered thiepane moiety and by C2 symmetry, were prepared. The complexes, related to the diamino cyclohexane family of platinum complexes, were soluble in dimethyl sulfoxide with the solvent substituting one chloride ion. These positively-charged complexes were tested against a human carcinoma cell line A431 and its cisplatin-resistant counterpart A431/Pt and were found to show: i) capability in bypassing cisplatin-resistance; ii) cytotoxicity comparable to that of oxaliplatin; iii) lower activity than cisplatin. In both cells lines, [PtCl(DACH)(DMSO)]+ was more cytotoxic than oxaliplatin. The best activity was shown by the platinum complexes with ligands which presented C2 symmetry.
authors.affiliation: Department of Organic Chemistry "A. Mangini", University of Bologna, Viale Risorgimento, 4, 40136 Bologna, Italy.
authors.forename: Vanda
authors.initials: V
authors.lastname: Cerè
authors.forename: Loris
authors.initials: L
authors.lastname: Grossi
authors.forename: Daniela
authors.initials: D
authors.lastname: Munari
authors.forename: Salvatore
authors.initials: S
authors.lastname: Pollicino
authors.forename: Laura
authors.initials: L
authors.lastname: Martelli
authors.forename: Mario
authors.initials: M
authors.lastname: Martelli
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008024:Ligands; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000077150:Oxaliplatin; D010087:Oxides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013846:Thiepins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands; D009944:Organoplatinum Compounds; D010087:Oxides; D013846:Thiepins; D000077150:Oxaliplatin; D002945:Cisplatin