Radiosensitization by derivatives of isoindole-4,7-dione.
New derivatives of isoindole -4,7-dione have been synthesized and their radiation sensitization and chemical behavior have been studied. One-electron reduction potentials have been determined by pulse radiolysis and found to be in the range of -0.45 to -0.36 V vs NHE . Radiosensitization effects were tested in vivo using soft tissue sarcoma transplanted in mice. All the isoindole -4,7-diones tested were found to exert considerable radiosensitization, approaching that of misonidazole tested under comparable conditions. The derivatives which contain a carbethoxy group on the pyrrolic ring were found to have more positive reduction potentials and to act as more efficient sensitizers. Further development of this class of radiosensitizers is underway.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D007211:Indoles / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity; D051379:Mice; D008807:Mice, Inbred BALB C; D008920:Misonidazole / Q000627:therapeutic use; D009368:Neoplasm Transplantation; D011675:Pulse Radiolysis; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity; D012513:Sarcoma, Experimental / Q000188:drug therapy / Q000532:radiotherapy*
D007211:Indoles; D011838:Radiation-Sensitizing Agents; D008920:Misonidazole