Chibber R, Stratford I J, Ahmed I, Robbins A B, Goodgame D, Lee B
Int J Radiat Oncol Biol Phys. 1984 Aug;10(8):1213-5. doi: 10.1016/0360-3016(84)90320-1.
Various transition metal complexes containing nitroimidazoles as ligands have been shown to act as radiosensitizers of hypoxic cells in vitro. Sensitization by cis-Pt(II)Cl2 (nitroimidazole)2 complexes is no greater than that which can be demonstrated by the free nitroimidazole ligand alone. These results differ from those previously described for the compound FLAP where an ER of 2.4 was obtained at a concentration of 50 microM. We report that, even using the same treatment technique, the maximum ER that can be achieved is 1.2. Further, the sensitizing efficiency of FLAP cannot be improved when cells are kept in contact with the compound for 12 hours in air prior to deoxygenation and irradiation. In contrast, Rh(II) complexes show much greater sensitization than can be obtained with the free ligand and these compounds are in turn more efficient sensitizers than the comparable Pt(II) complexes.
各种以硝基咪唑为配体的过渡金属配合物已被证明在体外可作为缺氧细胞的放射增敏剂。顺式 - Pt(II)Cl₂(硝基咪唑)₂配合物的增敏作用并不比单独使用游离硝基咪唑配体时更强。这些结果与之前描述的化合物FLAP的结果不同，在50微摩尔浓度下，FLAP的增强比为2.4。我们报道，即使使用相同的处理技术，所能达到的最大增强比也仅为1.2。此外，在脱氧和辐照前，若细胞在空气中与该化合物接触12小时，FLAP的增敏效率也无法提高。相比之下，Rh(II)配合物的增敏作用比游离配体强得多，并且这些化合物作为增敏剂比相应的Pt(II)配合物更有效。
