title: Platinum(IV) complex with adamantylamine as nonleaving amine group: synthesis, characterization, and in vitro antitumor activity against a panel of cisplatin-resistant cancer cell lines.
abstract: Procedure of the synthesis is described for new platinum(IV) drug LA-12 [(OC-6-43)-bis(acetato)(1-adamantylamine)amminedichloroplatinum(IV)]. The X-ray diffraction analysis shows that the structure is created by molecules with octahedral arrangement of ligands around a platinum atom and contains one H(2)O molecule that is not a part of the coordination sphere of platinum. This new drug is more reactive with glutathione than cisplatin and is lacking cross-resistance with cisplatin as proven on the panel of cancer cell lines.
authors.affiliation: PLIVA-Lachema a.s., Karásek 1, 62133 Brno, Czech Republic.
authors.forename: Frantisek
authors.initials: F
authors.lastname: Zák
authors.forename: Jaroslav
authors.initials: J
authors.lastname: Turánek
authors.forename: Ales
authors.initials: A
authors.lastname: Kroutil
authors.forename: Petr
authors.initials: P
authors.lastname: Sova
authors.forename: Adolf
authors.initials: A
authors.lastname: Mistr
authors.forename: Anna
authors.initials: A
authors.lastname: Poulová
authors.forename: Petr
authors.initials: P
authors.lastname: Mikolin
authors.forename: Zdirad
authors.initials: Z
authors.lastname: Zák
authors.forename: Andrea
authors.initials: A
authors.lastname: Kasná
authors.forename: Dana
authors.initials: D
authors.lastname: Záluská
authors.forename: Jirí
authors.initials: J
authors.lastname: Neca
authors.forename: Lenka
authors.initials: L
authors.lastname: Sindlerová
authors.forename: Alois
authors.initials: A
authors.lastname: Kozubík
mesh_terms: D000547:Amantadine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D018360:Crystallography, X-Ray; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C482801:bis(acetato)(1-adamantylamine)amminedichloroplatinum(IV); D000547:Amantadine; D002945:Cisplatin