Near-infrared (NIR) fluorophores have unique features that endow them with several advantages over conventional shorter wavelength emitting dyes. As a result, they have been widely utilized as fluorescence and photoacoustic imaging agents, as well as photodynamic and photothermal therapeutic agents. However, non-targeting NIR fluorescence-emitting organic molecules have the drawback of low selectivity toward tumors, which potentially results in severe side effects caused by damage to normal tissues. Thus, the development of NIR fluorophore-based substances that target tumors is a highly active area in medicinal chemistry research. Research efforts carried out thus far have led to the development of a number of NIR fluorophore-based, tumor imaging and therapeutic agents. The discussion in this review focuses on the results of research reported in the 2012–2021 period, giving particular emphasis to studies of NIR small organic dye-based imaging and therapeutic agents that are designed utilizing cancer-selective strategies.

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用于癌症成像和治疗的近红外 (NIR) 荧光发射有机小分子

近红外 (NIR) 荧光团具有独特的特性，与传统的较短波长发射染料相比，它们具有多种优势。因此，它们已被广泛用作荧光和光声成像剂，以及光动力和光热治疗剂。然而，非靶向近红外荧光发射有机分子具有对肿瘤选择性低的缺点，这可能导致对正常组织的损伤引起的严重副作用。因此，开发靶向肿瘤的基于 NIR 荧光团的物质是药物化学研究的一个高度活跃的领域。迄今为止进行的研究工作已导致开发了许多基于 NIR 荧光团的肿瘤成像和治疗剂。