1-取代苄氧基-3,6,7-三羟基-氧杂蒽酮的合成及NCI-H460细胞抑制活性研究

Synthesis of 1-substituted-benzyl-oxy-3,6,7-trihydroxyl xanthone with NCI-H460 cells inhibitory activity evaluation

目的对1-取代苄氧基-3,6,7-三羟基-氧杂蒽酮的苄基进行取代而合成8个化合物,研究此化合物对细胞产生毒性作用。方法设计合成8个氧杂蒽酮类化合物,用核磁技术进行确证;对其细胞毒活性做初步筛选。结果所合成的8个氧杂蒽酮类化合物均乃第一次报道,大多数目标化合物对NCI-H460肿瘤细胞活性有不同程度的抑制作用,其中化合物β、δ、ε和ζ作用较强。结论 R基团引入取代苄基形成的氧杂蒽酮类化合物具有抑制肿瘤细胞作用。

Objective To study the influence on cytotoxicity of 1- substituted- benzyl- oxy- 3,6,7- trihydroxyl xanthone inletting different benzyl groups. Methods Eight target compounds were designed and synthesized. All of them were confirmed by 1H- NMR spectra. Results Eight xanthone compounds were reported firstly. The results of preliminary pharmacological test showed that all the target compounds exhibited potent NCI- H460 cell inhibitory activity especially the compound β,δ,εand ζ. Conclusion R group of xanthone inletting benzyl synthesized compounds have inhibitory effect on tumor cells.