title: Synthesis and cytotoxic activities of estrone and estradiol cis-dichloroplatinum(II) complexes.
abstract: Sixteen platinum(II) complexes of estrone and estradiol were synthesized in this work to evaluate their cytotoxic activity against several cancer cell lines including estrogen dependent and independent ones. The synthesis of all the complexes was done in three steps. The reaction of steroids with dibromoalkanes was followed by a reaction of the bromoalkyl steroids with 2-(aminomethyl)pyridine or 2-(2-aminoethyl)pyridine. The last step was a reaction of steroidal diamino ligands with potassium tetrachloroplatinate to obtain the desired platinum(II) complexes. Cytotoxicity assays showed that most of the complexes prepared are active against the cancer cell lines used-CEM, U-2 OS, MCF7, MCF7 AL, MDA-MB-468, BT-474, BT-549, and BJ fibroblasts. The six-membered platinum complexes are more active than five-membered ones.
authors.affiliation: Institute of Organic Chemistry and Biochemistry ASCR, Flemingovo n. 2, 16610 Prague 6, Czech Republic. kvasnica@uochb.cas.cz
authors.forename: Miroslav
authors.initials: M
authors.lastname: Kvasnica
authors.forename: Lucie
authors.initials: L
authors.lastname: Rarova
authors.forename: Jana
authors.initials: J
authors.lastname: Oklestkova
authors.forename: Milos
authors.initials: M
authors.lastname: Budesinsky
authors.forename: Ladislav
authors.initials: L
authors.lastname: Kohout
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004970:Estrone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D061986:MCF-7 Cells; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008024:Ligands; D009944:Organoplatinum Compounds; D004970:Estrone; D004958:Estradiol