a Ecole de Biologie Industrielle, EBInnov , Cergy-Pontoise , France.
b Faculté de Pharmacie - ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453 - INSERM US7, Université de Lyon, Université Claude Bernard Lyon 1 , Lyon , France.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):1321-1346. doi: 10.1080/14756366.2019.1640692.
For over half a century, the carbazole skeleton has been the key structural motif of many biologically active compounds including natural and synthetic products. Carbazoles have taken an important part in all the existing anti-cancer drugs because of their discovery from a large variety of organisms, including bacteria, fungi, plants, and animals. In this article, we specifically explored the literature from 2012 to 2018 on the anti-tumour activities reported to carbazole derivatives and we have critically collected the most significant data. The most described carbazole anti-tumour agents were classified according to their structure, starting from the tricyclic-carbazole motif to fused tetra-, penta-, hexa- and heptacyclic carbazoles. To date, three derivatives are available on the market and approved in cancer therapy.
半个多世纪以来，咔唑骨架一直是许多具有生物活性的化合物的关键结构基序，包括天然产物和合成产物。由于从包括细菌、真菌、植物和动物在内的各种生物体中发现了咔唑，因此它在所有现有的抗癌药物中都占有重要地位。在本文中，我们专门研究了 2012 年至 2018 年关于报道的咔唑衍生物的抗肿瘤活性的文献，并批判性地收集了最重要的数据。根据结构，将最描述的咔唑抗肿瘤剂进行了分类，从三环咔唑基序到融合的四、五、六和七元环咔唑。迄今为止，已有三种衍生物在市场上销售并批准用于癌症治疗。
