Synthesis and antitumor activity of some aromatic seleno lactones.
Several aromatic seleno lactones have been synthesized and shown to possess significant inhibitory activity against human colon tumor-8r cells in culture at concentrations lower than 1 mM. Although all of the compounds tested were found to be active, 5-hydroxy-3-[(phenylseleno)methyl]hydrocoumarinoctanoate (3d) and 5-hydroxy-3-[(phenylseleno)methyl]hydrocoumarindecanoate (3e) were found to be the most effective in inhibiting cell growth. In situ formation of the corresponding alpha-methylene lactones is postulated to account for the cytotoxic activity in this class of compounds.
D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms; D003374:Coumarins / Q000138:chemical synthesis* / Q000633:toxicity; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D012643:Selenium / Q000138:chemical synthesis* / Q000633:toxicity; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D003374:Coumarins; D007202:Indicators and Reagents; D012643:Selenium