title: Synthesis and in vitro characterization of platinum(II) anticancer coordinates using FTIR spectroscopy and NCI COMPARE: A fast method for new compound discovery.
abstract: Platinum-based drugs have been used for several decades to treat various cancers successfully. Cisplatin is the original compound in this class; it cross-links DNA, resulting in cell cycle arrest and cell death via apoptosis. Cisplatin is effective against several tumor types but exhibits toxic side effects; in addition, tumors often develop resistance. An original in vitro approach is proposed to determine whether platinum-based research compounds are good candidates for further study by comparing them to marketed drugs using FTIR spectroscopy and the COMPARE analysis from the NCI. Both methods can produce fingerprints and highlight differences between the compounds, classifying the candidates and revealing promising derivatives.
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Campus Plaine CP205/5, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium. Electronic address: giberger@ulb.ac.be.
authors.forename: Gilles
authors.initials: G
authors.lastname: Berger
authors.affiliation: Laboratoire de Toxicologie et Cancérologie Expérimentale, Faculté de Pharmacie, Campus Plaine CP205/1, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Hélène
authors.initials: H
authors.lastname: Leclercqz
authors.affiliation: Center for Structural Biology and Bioinformatics, Laboratory for the Structure and Function of Biological Membranes, Campus Plaine CP206/2, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Allison
authors.initials: A
authors.lastname: Derenne
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Campus Plaine CP205/5, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Michel
authors.initials: M
authors.lastname: Gelbcke
authors.affiliation: Center for Structural Biology and Bioinformatics, Laboratory for the Structure and Function of Biological Membranes, Campus Plaine CP206/2, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Erik
authors.initials: E
authors.lastname: Goormaghtigh
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Campus Plaine CP205/5, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Jean
authors.initials: J
authors.lastname: Nève
authors.affiliation: Laboratoire de Toxicologie et Cancérologie Expérimentale, Faculté de Pharmacie, Campus Plaine CP205/1, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: Véronique
authors.initials: V
authors.lastname: Mathieu
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Campus Plaine CP205/5, Université Libre de Bruxelles, Bd du Triomphe, B1050 Brussels, Belgium.
authors.forename: François
authors.initials: F
authors.lastname: Dufrasne
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004354:Drug Screening Assays, Antitumor; D005434:Flow Cytometry; D006801:Humans; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds
keywords: COMPARE; Chemotherapy; Cytotoxicity; Infrared spectroscopy; NCI; Platinum