Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Chemistry, Faculty of Health Science , Thessaloniki 54124 , Greece.
Expert Opin Ther Pat. 2014 Dec;24(12):1323-47. doi: 10.1517/13543776.2014.972368. Epub 2014 Oct 18.
Coumarins belong to the benzopyrones family. They are naturally plant-derived and synthetically taken polyphenolic substances, presenting a wide variety of biological activities and behaviours, supporting their use as therapeutic agents for multiple diseases. Their structural characteristics correlated to physicochemical properties seem to define the extent of the biological activity.
Recent patent publications (2012-2014), describing coumarins and their derivatives are analyzed. Synthesis, hybridization techniques and biological evaluation in vitro/in vivo, for example, antimitotic, antiviral, anticancer, cytotoxic, anti-acne and antioxidant coumarin macromolecule polymer agents are included. Furthermore, a wide range of pharmaceutical applications and pharmaceutical compositions are also summarized.
Several natural and synthetic coumarins, hybrids and derivatives appear to have promising anticancer-antitumor activities. Their clinical evaluation will be critical to assess therapeutic utility. The compounds for which the mechanism of action is well defined can serve as lead compounds for the design of new more potent molecules.
香豆素属于苯并吡喃酮家族。它们是天然植物衍生和人工合成的多酚类物质，具有广泛的生物活性和行为，支持将其用作多种疾病的治疗剂。其与物理化学性质相关的结构特征似乎决定了生物活性的程度。
分析了最近（2012-2014 年）的专利出版物，描述了香豆素及其衍生物。包括合成、杂交技术和体外/体内的生物评价，例如抗有丝分裂、抗病毒、抗癌、细胞毒性、抗痤疮和抗氧化香豆素大分子聚合物剂。此外，还总结了广泛的药物应用和药物组合物。
几种天然和合成的香豆素、杂种和衍生物似乎具有有前途的抗癌抗肿瘤活性。对其进行临床评估对于评估治疗效果至关重要。对于作用机制明确的化合物，可以作为设计新型更有效分子的先导化合物。
