title: Synthesis of 9-acridinyl sulfur derivatives: sulfides, sulfoxides and sulfones. Comparison of their activity on tumour cells.
abstract: The synthesis of several acridine thioethers is described. These compounds were oxidized to give new sulfoxides and sulfones. Among 23 compounds prepared, 19 were tested in vitro against the human cancer cell lines panel of NCI screening. Activity is increased 5-10 times from sulfides to sulfoxides. Among substituted groups in the side chain, sulfur mustard, epoxy sulfide and sulfoxide displayed the most interesting activity.
authors.affiliation: GERCTOP-UMR CNRS 6009, faculté de pharmacie, université de la Méditerranée, 27, boulevard Jean Moulin, 13385 Marseille 5, France. christiane.santelli@pharmacie.univ-mrs.fr
authors.forename: Christiane
authors.initials: C
authors.lastname: Santelli-Rouvier
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Barret
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Farrell
authors.forename: Derek
authors.initials: D
authors.lastname: Sharples
authors.forename: Bridget T
authors.initials: BT
authors.lastname: Hill
authors.forename: Jacques
authors.initials: J
authors.lastname: Barbe
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004249:DNA Damage / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis* / Q000494:pharmacology; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology; D013454:Sulfoxides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D013440:Sulfides; D013450:Sulfones; D013454:Sulfoxides