布洛酚—邻氨基苯酚衍生物的合成及酪氨酸酶催化的释放研究

Model Prodrug for Treatment of Malignant Melanoma: Designed and Synthesis of o-Aminophenol Derivative

设计并合成了邻氨基酚布洛酚酯,根据推论的酪氨酸酶催化反应机理,进行了模拟实验研究。邻氨基酚布洛酚酯在酪氨酸酶和芳香胺存在下,发生了氧化、加成和取代反应,实现了布洛酚的释放,表明该设计在黑色瘤治疗中的潜在应用前景。

A novel model prodrug of o-aminophenol derivative was designed and synthesized and functioned as a tyrosinase substrate to allow treatment of malignant melanoma. After being catalyzed by tyrosinase and aromatic amine, the reaction product and HPLC analysis indicate that this agent has been evaluated for tyrosinase-mediated drug release, and shown to act in the desired manner.