Dichiara Maria, Prezzavento Orazio, Marrazzo Agostino, Pittalà Valeria, Salerno Loredana, Rescifina Antonio, Amata Emanuele
Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy.
Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy.
Eur J Med Chem. 2017 Dec 15;142:459-485. doi: 10.1016/j.ejmech.2017.08.070. Epub 2017 Sep 4.
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.
在寻找癌症治疗新策略的过程中，光动力疗法（PDT）已成为一种有效、可重复安全使用且非侵入性的方法。该技术涉及使用两种主要的无毒成分，一种光敏剂（PS）和一个可见光或近红外（NIR）光源，二者结合以氧依赖或非依赖的方式诱导细胞损伤。涉及卟啉及其衍生物的大环化合物是PDT中使用的主要一类PS剂。然而，由于与这些PS相关的缺点，如光敏感性、暗毒性和低波长吸收率，似乎需要新型的PS。本综述总结了作为PDT中抗癌治疗剂的非卟啉类PS药物发现的最新进展。不同的化合物按化学类别分组，并就光毒性以及设计的关键方面和构效关系进行了讨论。
