Infante G A, Guzman P, Alvarez R, Figueroa A, Correa J N, Myers J A, Lanier L J, Williams T M, Burgos S, Vera J
Radiat Res. 1984 May;98(2):234-41.
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.
已合成异吲哚 -4,7-二酮的新衍生物，并对其辐射增敏作用和化学行为进行了研究。通过脉冲辐解测定了单电子还原电位，发现相对于标准氢电极，其范围为-0.45至-0.36V。使用移植于小鼠的软组织肉瘤在体内测试了辐射增敏效果。发现所有测试的异吲哚 -4,7-二酮均具有相当大的辐射增敏作用，接近在可比条件下测试的米索硝唑的增敏作用。发现吡咯环上含有乙氧羰基的衍生物具有更正的还原电位，并且作为更有效的增敏剂。这类辐射增敏剂的进一步研发正在进行中。
