title: Fourier transform infrared (FTIR) spectroscopy to monitor the cellular impact of newly synthesized platinum derivatives.
abstract: Platinum complexes remain widely used to combat various types of cancers. Three platinum complexes, cisplatin, carboplatin and oxaliplatin, are marketed for various oncological purposes. Additionally, nedaplatin, lobaplatin and heptaplatin have gained regionally limited approval for oncology purposes. Furthermore, various platinum derivatives are currently under clinical trials. More than 40 years after their discovery, however, the precise mechanism of action of platinum antitumor complexes remains elusive, partly because these compounds display numerous intracellular targets. Structure-activity-relationship analyses are therefore difficult to conduct to optimize the synthesis of novel platinum derivatives. The aim of the present study is to illustrate the potential of using Fourier Transform Infrared (FTIR) analyses to monitor the cellular modifications induced by the new platinum derivatives that we have synthesized. We show in the present study the advantages of combining an in vitro assay to determine the IC50 growth inhibition concentrations of a series of compounds belonging to a given chemical series and FTIR analyses carried out at the IC50 concentrations for each compound to identify potential hits within this series of compounds. The original pharmacological approach proposed here could, therefore, avoid large-scale pharmacological experiments to find hits within a given chemical series.
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Institut de Pharmacie, Faculty of Sciences, Université Libre de Bruxelles (ULB), Brussels, Belgium.
authors.forename: Gilles
authors.initials: G
authors.lastname: Berger
authors.forename: Régis
authors.initials: R
authors.lastname: Gasper
authors.forename: Delphine
authors.initials: D
authors.lastname: Lamoral-Theys
authors.forename: Anja
authors.initials: A
authors.lastname: Wellner
authors.forename: Michel
authors.initials: M
authors.lastname: Gelbcke
authors.forename: Ronald
authors.initials: R
authors.lastname: Gust
authors.forename: Jean
authors.initials: J
authors.lastname: Nève
authors.forename: Robert
authors.initials: R
authors.lastname: Kiss
authors.forename: Erik
authors.initials: E
authors.lastname: Goormaghtigh
authors.forename: François
authors.initials: F
authors.lastname: Dufrasne
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods*
chemical_list: D009944:Organoplatinum Compounds