In the search of novel strategies for the treatment of cancer, photodynamic therapy (PDT) has emerged as an effective, safe for repeated use, and non-invasive method. This technique involves the use of two major non-toxic components, a photosensitizer (PS) and a visible or near-infrared (NIR) light source, combined to induce cellular damage in an oxygen-dependent or -independent manner. Macrocyclic compounds, involving porphyrin and their derivatives, represent the major class of PS agents used in PDT. However, due to the drawbacks associated with these PS, like photosensitivity, dark toxicity, and low wavelength absorbance, new classes of PS appear to be needed. This review summarizes over the recent advances in drug discovery of non-porphyrinic PS suitable as anticancer therapeutics in PDT. The different compounds are grouped by chemical classes and discussed in terms of phototoxicity, together with the critical aspects of design and structure-activity relationship.

在寻找新的癌症治疗策略时，光动力疗法（PDT）已成为一种有效，可重复使用且安全的非侵入性方法。该技术涉及使用两种主要的无毒成分，即光敏剂（PS）和可见光或近红外（NIR）光源，两者结合以氧依赖性或非依赖性方式诱导细胞损伤。涉及卟啉及其衍生物的大环化合物代表了PDT中使用的PS试剂的主要类别。但是，由于与这些PS相关的缺点，例如光敏性，暗毒性和低波长吸收率，因此似乎需要新的PS类。这篇综述总结了非卟啉PS作为PDT中的抗癌治疗剂的药物发现的最新进展。