吡啶丙烯酰氨基酸衍生物的设计、合成及其对离体HeLa-S3细胞的放射增敏作用

本文设计、合成了一类新型的放射增敏剂—吡啶丙烯酰氨基酸衍生物,并测定了对HeLa-Sa细胞的增敏作用和细胞毒性。3-吡啶丙烯酰甲基甘氨酸(3A)和4-吡啶丙烯酰甲基甘氨酸(4A)的主要作用分别为减小细胞存活曲线的肩宽和Do值。这类化合物,尤其是3A和4A,或其结构类似物,如果体内实验证明有明显增敏作用,将有重要的潜在临床应用价值。

DESIGN AND SYNTHESIS OF N-(PYRIDYLACRYL) AMINO ACID DERIVATIVES AS POTENTIAL RADIOSENSITIZERS AGAINST HELA-S3 CELLS IN VITRO

A new series of N-(pyridylacryl) amino acid derivatives have been designed and synthesized as potential radiosensitizers in an effort to increase therapeutic efficacy with less toxicity. Radiosensitization and cytotoxicity of the newly synthesized compounds upon HeLa-S₃ cells were measured. The main effects of the reduction of the shoulder width and Do value of the survival curve by 3-pyridylacrylsarcosine (3A) and 4-pyridylacrylsarcosine (4A) were observed. This work has demonstrated that this series of compounds, especially 3A and 4A, or their structurally related compounds, showed great clinical potential as radiosensitizers if significant radiosensitizing activity in vivo could be achieved.