title: New approach for the preparation of efficient DNA cleaving agents: ditopic copper-platinum complexes based on 3-Clip-Phen and cisplatin.
abstract: The design and synthesis of new heterodinuclear DNA-targeting agents are described. The abilities of cisplatin and Cu(3-Clip-Phen) [Cu(1-(1,10-phenanthrolin-3-yloxy)-3-(1,10-phenanthrolin-8-yloxy)propan-2-amine)Cl2], an artificial DNA-cleaving agent, have been combined through their "covalent coupling". This strategy has led to bifunctional complexes that are able to cleave the DNA in a double-stranded fashion in contrast to Cu(3-Clip-Phen) alone and have promising cytotoxicities compared to cisplatin in several cell lines.
authors.affiliation: Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, Post Office Box 9502, 2300 RA Leiden, The Netherlands.
authors.forename: Paul de
authors.initials: Pd
authors.lastname: Hoog
authors.forename: Christophe
authors.initials: C
authors.lastname: Boldron
authors.forename: Patrick
authors.initials: P
authors.lastname: Gamez
authors.forename: Karen
authors.initials: K
authors.lastname: Sliedregt-Bol
authors.forename: Isabelle
authors.initials: I
authors.lastname: Roland
authors.forename: Marguerite
authors.initials: M
authors.lastname: Pitié
authors.forename: Robert
authors.initials: R
authors.lastname: Kiss
authors.forename: Bernard
authors.initials: B
authors.lastname: Meunier
authors.forename: Jan
authors.initials: J
authors.lastname: Reedijk
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D053837:DNA Cleavage; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; C531042:dichloro(1-(1,10-phenanthrolin-3-yloxy)-3-(1,10-phenanthrolin-8-yloxy)propane-2-amine)copper(II); D002945:Cisplatin