Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123, Palermo, Italy.
Telethon Institute of Genetics and Medicine (TIGEM), Campi Flegrei 34, 80078, Pozzuoli, NA, Italy.
Eur J Med Chem. 2019 Oct 15;180:283-290. doi: 10.1016/j.ejmech.2019.07.025. Epub 2019 Jul 10.
Multi-target molecular entities, offer a path to progress both in understanding causes of disease and in defining effective small molecule treatments. Coumarin and its derivatives belong to an important group of natural compounds with diverse biological properties. They are found in vegetables and plants for which literature reports thousands of publications for the great variety of biological applications among which the photoprotective effects, thus being considered multi-targeting agents. Their furan condensed analogues constitute the family of furocoumarins, less represented in the literature, endowed with photosensitizing properties and often used for the treatment of skin diseases such as vitiligo and psoriasis. Despite the study of biological properties of linear and angular furocumarins dates back to ancient times, mainly as photosensitizers, these small molecules still represent an attractive scaffold for further development and applications in several therapeutic fields. The aim of the present review is to summarize the most promising chemical entities belonging to the class of furocumarins and coumarins, emerged in the last decades, and the methods used for their synthesis with a particular focus on main targets involved in the cystic fibrosis treatment.
多靶点分子实体为深入了解疾病的病因和确定有效的小分子治疗方法提供了一条途径。香豆素及其衍生物属于具有多种生物特性的天然化合物的重要类别。它们存在于蔬菜和植物中，文献中报道了数千篇关于其广泛生物应用的文章，其中包括光保护作用，因此被认为是多靶点药物。它们的呋喃稠合类似物构成了呋喃香豆素家族，在文献中较少被报道，具有光敏特性，常用于治疗白癜风和牛皮癣等皮肤病。尽管线性和角型呋喃香豆素的生物特性研究可以追溯到古代，主要作为光敏剂，但这些小分子仍然是进一步开发和应用于多个治疗领域的有吸引力的支架。本文综述了过去几十年中出现的最有前途的属于呋喃香豆素和香豆素类的化学实体，以及用于其合成的方法，特别关注了参与囊性纤维化治疗的主要靶点。
