Fluorophores are essential tools for optical imaging and biomedical research. Their synthetic modification to incorporate new functions, however, remains a challenging task. Conventional strategies rely on linear synthesis in which a parent framework is gradually extended. We here designed and synthesized a versatile library of multi‐functional fluorophores via a scaffold‐based Ugi four‐component reaction (U‐4CR). The adaptability of the scaffold is achieved through modification of starting materials. This allows to use a small range of starting materials for the creation of fluorogenic probes that can detect reactive‐oxygen species and where the localization into subcellular organelles or membranes can be controlled. We present reaction yields ranging from 60 % to 90 % and discovered that some compounds can even function as imaging and therapeutic agents via Fenton chemistry inducing pyroptosis in living cancer cells. Our study underlines the potential of scaffold‐based synthesis for versatile creation of functional fluorophores and their applications.

中文翻译：

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用于靶向细胞成像和焦亡的多功能荧光基团的模块化设计和支架合成


荧光基团是光学成像和生物医学研究的重要工具。然而，它们为加入新功能而进行合成改性仍然是一项具有挑战性的任务。传统策略依赖于线性综合，其中父框架逐渐扩展。我们在这里通过基于支架的 Ugi 四组分反应 （U-4CR） 设计并合成了一个多功能荧光团库。支架的适应性是通过对起始材料的改性来实现的。这允许使用少量的起始材料来创建荧光探针，这些探针可以检测反应氧，并且可以控制定位到亚细胞器或膜中。我们提出了 60 % 到 90 % 的反应产率，并发现一些化合物甚至可以通过 Fenton 化学在活癌细胞中诱导焦亡，从而起成像和治疗剂的作用。我们的研究强调了基于支架的合成在多功能创建功能性荧光团及其应用方面的潜力。