Synthesis and evaluation of novel caged DNA alkylating agents bearing 3,4-epoxypiperidine structure
作者:Yuji Kawada、Tetsuya Kodama、Kazuyuki Miyashita、Takeshi Imanishi、Satoshi Obika
DOI:10.1039/c2ob25366f
日期:——
Previously, we reported that the 3,4-epoxypiperidine structure, whose design was based on the active site of DNA alkylating antitumor antibiotics, azinomycins A and B, possesses prominent DNA cleavage activity. In this report, novel caged DNA alkylating agents, which were designed to be activated by UV irradiation, were synthesized by the introduction of four photo-labile protecting groups to a 3,4-epoxypiperidine
以前,我们报道了3,4-环氧哌啶结构(其设计基于DNA烷基化抗肿瘤抗生素,阿奇霉素A和B的活性位点)具有突出的DNA裂解活性。在本报告中,通过将三个对光不稳定的保护基团引入3,4-环氧哌啶衍生物中,合成了设计用于UV辐射活化的新型笼状DNA烷基化剂。笼罩的DNA烷化剂的DNA切割活性和细胞毒性在紫外线照射下进行了检查。根据保护基的光敏性,四种笼中的DNA烷基化剂显示出不同程度的生物活性。