A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.
使用1,2,4-苯并
三氮唑氧化物的方法,其中一些是新颖的化合物,作为放射增敏剂和选择性细胞毒性剂的方法被揭示。这些化合物被证明能够特异性地增敏缺氧肿瘤细胞。其中一些还被揭示为这些细胞的特异性细胞毒性剂。它们还表现出在用药物处理细胞之前或之后的缺氧培养后,对好氧细胞具有意外的增敏能力。这为相对于正常细胞的肿瘤选择性增敏提供了基础。还揭示了一种制备1,2,4-苯并
三氮唑氧化物的新方法。