Synthesis of 9-acridinyl sulfur derivatives: sulfides, sulfoxides and sulfones. Comparison of their activity on tumour cells.
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.
Santelli-Rouvier
Christiane
C
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
Barret
Jean-Marc
JM
Farrell
Christopher M
CM
Sharples
Derek
D
Hill
Bridget T
BT
Barbe
Jacques
J
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
D000970:Antineoplastic Agents; D013440:Sulfides; D013450:Sulfones; D013454:Sulfoxides