萘酰亚胺多胺衍生物的合成及其抗肿瘤活性

摘要

A series of polyamine derivatives of naphthalimide(3a~3d) to be used as antitumor agents was synthesized. The biological and spectroscopic evaluations showed that compounds 3a ~ 3d could used as DNA intercalators and had stronger cytotoxic activity and better selectivity than those of amonafide against cancer cells in vitro. The IC50 for antiproliferative activity of compound 3b on four cancer cells were 7. 80, 5. 08, 9.78 and 9. 27 μmol/L, respectively. High content screening ( HCS) results revealed that the as-prepared compounds might produce cytotoxicity through apoptosis via mitochondrial pathway.%设计合成了萘酰亚胺的4种新的多胺衍生物并进行了体外抗肿瘤活性测试.结果表明,这些萘酰亚胺衍生物能够嵌入DNA碱基对中,并且比氨萘非特对肿瘤细胞具有更高的毒性和更好的选择性,其中化合物3b对4种肿瘤细胞的抑制IC50值分别为7.80、5.08、9.78和9.27 μmol/L;高内涵活细胞成像系统结果显示,这些化合物可能是通过线粒体通路而导致的细胞凋亡.