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Exploiting azide-alkyne click chemistry in the synthesis, tracking and targeting of platinum anticancer complexes.
Current Opinion in Chemical Biology ( IF 7.8 ) Pub Date : 2020-01-13 , DOI: 10.1016/j.cbpa.2019.12.001
Nicola J Farrer 1 , Darren M Griffith 2
Affiliation  

Click chemistry is fundamentally important to medicinal chemistry and chemical biology. It represents a powerful and versatile tool, which can be exploited to develop novel Pt-based anticancer drugs and to better understand the biological effects of Pt-based anticancer drugs at a cellular level. Innovative azide-alkyne cycloaddition-based approaches are being used to functionalise Pt-based complexes with biomolecules to enhance tumour targeting. Valuable information in relation to the mechanisms of action and resistance of Pt-based drugs is also being revealed through click-based detection, isolation and tracking of Pt drug surrogates in biological and cellular environments. Although less well-explored, inorganic Pt-click reactions enable synthesis of novel (potentially multimetallic) Pt complexes and provide plausible routes to introduce functional groups and monitoring Pt-azido drug localisation.

中文翻译:

在铂类抗癌复合物的合成,跟踪和靶向中利用叠氮化物-炔烃点击化学。

点击化学对药物化学和化学生物学至关重要。它代表了功能强大且用途广泛的工具,可用于开发新颖的基于Pt的抗癌药,并在细胞水平上更好地了解基于Pt的抗癌药的生物学作用。创新的基于叠氮化物-炔烃环加成的方法正被用于功能化基于Pt的复合物与生物分子,以增强肿瘤靶向性。还通过在生物和细胞环境中基于点击的检测,分离和追踪Pt替代药物来揭示与Pt药物的作用机制和耐药性有关的重要信息。尽管探索程度较差,
更新日期:2020-01-13
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