title: Combinatorial discovery of new asymmetric cis platinum anticancer complexes is made possible with solid-phase synthetic methods.
abstract: To efficiently access asymmetric cis platinum (II) complexes for biological evaluation, a new solid-phase synthesis was designed. This synthesis was used for the preparation of a small library of platinum compounds. Several compounds from this library revealed promising activity during a cytotoxicity screen. Two active compounds were, therefore, synthesised on a larger scale and tested more extensively against a larger panel of cell-lines, confirming their high potential as antitumour compounds. The work presented illustrates how a combination of a new methodology and established techniques can speed up the search for platinum complexes with improved cytotoxic profiles compared to cisplatin.
authors.affiliation: Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands.
authors.forename: Steven
authors.initials: S
authors.lastname: van Zutphen
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Stone
authors.forename: Sabine
authors.initials: S
authors.lastname: van Rijt
authors.forename: Marc S
authors.initials: MS
authors.lastname: Robillard
authors.forename: Gijs A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
authors.forename: Hans
authors.initials: H
authors.lastname: den Dulk
authors.forename: Jaap
authors.initials: J
authors.lastname: Brouwer
authors.forename: Jan
authors.initials: J
authors.lastname: Reedijk
mesh_terms: D002945:Cisplatin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D017671:Platinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D017671:Platinum Compounds; D002945:Cisplatin