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一种基于偶氮苯的杂合前药,通过调节亚细胞定位实现缺氧激活化疗。

An azobenzene-based heteromeric prodrug for hypoxia-activated chemotherapy by regulating subcellular localization.

机构信息

Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, P. R. China.

出版信息

Chem Commun (Camb). 2018 Jul 12;54(57):7983-7986. doi: 10.1039/c8cc03430c.

Abstract

An azobenzene-based heteromeric prodrug (hNDP) was prepared for targeted chemotherapy against hypoxic tumor. hNDP could divert the parent drug from nucleus to cytoplasm with lower toxicity, while the azoreduction of hNDP in hypoxia would activate the drug with a robust anti-tumor effect by initiating the apoptosis-related biochemical cascades.

摘要

一种基于偶氮苯的杂合前药 (hNDP) 被制备用于针对缺氧肿瘤的靶向化疗。hNDP 可以将亲代药物从细胞核转移到细胞质,毒性更低,而在缺氧条件下 hNDP 的偶氮还原会通过启动与细胞凋亡相关的生化级联反应来激活药物,从而产生强大的抗肿瘤作用。

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