Various radiosensitizers are being developed to increase the radiation sensitivity of hypoxic cancer cells, which show resistance to radiation. Previously, we demonstrated that an acetyl glucose-modified nitroimidazole derivative showed a high radiosensitizing effect by inhibiting glucose uptake and glycolysis. Based on this finding, we designed and synthesized novel sugar hybrid radiosensitizers, wherein acetyl glucose was introduced into gefitinib. Among them, UTX-114 had higher autophosphorylation and radiosensitizing activity than gefitinib and inhibited glucose uptake. This result supports our hypothesis that an acetyl glucose moiety improves the radiosensitizing effect of the drug, and UTX-114 can be expected to be a leading compound with a radiosensitizing effect.

正在开发各种放射增敏剂以增加低氧癌细胞的放射敏感性，所述低氧癌细胞显示出对放射的抗性。以前，我们证明了乙酰葡萄糖修饰的硝基咪唑衍生物通过抑制葡萄糖的摄取和糖酵解显示出高的放射增敏作用。基于这一发现，我们设计并合成了新型糖杂放射增敏剂，其中将乙酰葡萄糖引入吉非替尼。其中，UTX-114具有比吉非替尼更高的自磷酸化和放射增敏活性，并抑制了葡萄糖的摄取。该结果支持了我们的假设，即乙酰葡萄糖部分可改善药物的放射增敏作用，而UTX-114有望成为具有放射增敏作用的主要化合物。