H2O2-TYR级联激活前药的设计合成及抗癌活性研究
esign, synthesis and anticancer activity of prodrugs by H2O2-TYR cascade activation
黑色素瘤中同时过表达活性氧(ROS)和酪氨酸酶（TYR），利用这两种生物因子为激活剂，设计合成了H2O2-TYR级联激活的喹唑啉酮-芳基硼酸酯前药3和线粒体靶向前药4，以及TYR单激活前药5。所有化合物结构通过NMR和ESI-MS表征，用HPLC验证前药3对H2O2的响应行为。细胞毒性实验发现，线粒体靶向前药4与非靶向前药3、5相比，其对黑色素瘤细胞表现出增强的抗癌活性。
Both reactive oxygen species(ROS) and tyrosinase (TYR) are overexpressed in melanoma, so these two biomarkers can be used as activators to design H2O2-TYR cascade activated prodrugs. To this end, a quinazolinone-arylborate prodrug 3, a mitochondrial targeting prodrug 4 and a TYR single activated prodrug 5 were synthesized. All the compounds were characterized by NMR and ESI-MS, and the response behavior of prodrug 3 to H2O2 was verified by HPLC. Cytotoxicity results showed that compared with non-targeted prodrugs 3 and 5, mitochondrial targeted prodrug 4 showed enhanced anti-cancer activity on melanoma cells.?
黄静、黄佩玲
药学肿瘤学生物化学
靶向前药双重激活前药黑色素瘤喹唑啉酮-芳基硼酸酯衍生物
targeted prodrugsmultiple activation prodrugsmelanomaquinazolinone-aryl borate derivatives??
黄静,黄佩玲.H2O2-TYR级联激活前药的设计合成及抗癌活性研究[EB/OL].(2021-05-19)[2025-08-21].http://www.paper.edu.cn/releasepaper/content/202105-131.点此复制
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