Department of Organic Chemistry, NCCR Chemical Biology, Faculty of Sciences, University of Geneva, 1211, Geneva, Switzerland.
Angew Chem Int Ed Engl. 2022 Jul 11;61(28):e202203390. doi: 10.1002/anie.202203390. Epub 2022 May 20.
A Ru(bpy) Cl photocatalyst is applied to the rapid trans to cis isomerization of a range of alkene-containing pharmacological agents, including combretastatin A-4 (CA-4), a clinical candidate in oncology, and resveratrol derivatives, switching their configuration from inactive substances to potent cytotoxic agents. Selective in cellulo activation of the CA-4 analog Res-3M is demonstrated, along with its potent cytotoxicity and inhibition of microtubule dynamics.
一种 Ru(bpy)Cl 光催化剂被应用于一系列含有烯烃的药物的快速顺反异构化，包括在肿瘤学中有临床应用前景的 Combretastatin A-4（CA-4）和白藜芦醇衍生物，将它们的结构从无活性物质转化为有效的细胞毒性剂。我们证明了 CA-4 类似物 Res-3M 的选择性细胞内激活，以及它的强大的细胞毒性和对微管动力学的抑制作用。
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