光控抗肿瘤药物的合成

Synthesis of Photocage Antitumor Drugs

基于光响应开关的特性,我们使用邻硝基苄基类化合物作为开关,探究了硝基苄基光响应释放药物系统。以丝氨醇和炔丙胺为连接体,香兰素为原料,合成硝基苄基光响应开关。以青蒿琥酯为被释放基团,设计合成光控释放的青蒿琥酯药物。在通过紫外光320 nm波长照射下出现断键释放变化,建立紫外吸收峰模型,而对于青蒿琥酯进行光照射没有出现吸收峰变化。

Based on the characteristics of photoresponsive switches,we used o-nitrobenzyl compounds as switches to explore the photoresponsive drug delivery system.Nitrobenzyl photoresponsive switch was synthesized by using serine and propargyl alcohol as linkers and vanillin as raw materials.Artesunate was used as the released group to design and synthesize the light controlled drug.The UV absorption peak model was established by the change of bond breaking release under UV irradiation at 320 nm,but there was no change in the absorption peak of artesunate under UV irradiation.