Laboratorio de Patología y Farmacología Molecular, Instituto de Biología y Medicina Experimental, Vuelta de Obligado 2490. C1428DN, Buenos Aires, Argentina.
Curr Med Chem. 2010;17(13):1325-38. doi: 10.2174/092986710790936284.
Natural as well as synthetic coumarins have recently drawn much attention due to its broad pharmacological activities. Many coumarins and their derivatives exert anti-coagulant, anti-tumor, anti-viral, anti-inflammatory and anti-oxidant effects, as well as anti-microbial and enzyme inhibition properties. The recognition of key structural features within coumarin family is crucial for the design and development of new analogues with improved activity and for the characterization of their mechanism of action and potential side effects. The different substituents in the coumarin nucleus strongly influence the biological activity of the resulting derivatives. Although some coumarins have been already characterized to evoke a particular biological activity, the challenge would be the design and synthesis of new derivatives with high specific activity for other pharmacological targets and define their mechanism of action to achieve new therapeutic drugs. The present review highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anti-cancer agents. The major challenges about coumarins include the translation of current knowledge into new potential lead compounds and the repositioning of known compounds for the treatment of cancer.
天然和合成香豆素由于其广泛的药理学活性，最近引起了广泛关注。许多香豆素及其衍生物具有抗凝血、抗肿瘤、抗病毒、抗炎和抗氧化作用，以及抗菌和酶抑制特性。识别香豆素家族中的关键结构特征对于设计和开发具有改善活性的新类似物以及表征其作用机制和潜在副作用至关重要。香豆素核中的不同取代基强烈影响所得衍生物的生物活性。尽管已经有一些香豆素被表征为具有特定的生物活性，但挑战将是设计和合成具有针对其他药理靶点的高特异性活性的新型衍生物，并确定其作用机制以获得新的治疗药物。本综述强调了香豆素骨架作为新型抗癌药物在药物发现中的最新进展。香豆素面临的主要挑战包括将现有知识转化为新的潜在先导化合物，以及重新定位已知化合物以治疗癌症。
