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咔唑骨架在癌症治疗中的应用:2012 年至 2018 年的综述。

Carbazole scaffolds in cancer therapy: a review from 2012 to 2018.

机构信息

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.

出版信息

J Enzyme Inhib Med Chem. 2019 Dec;34(1):1321-1346. doi: 10.1080/14756366.2019.1640692.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b98/6691762/0236e58b4f92/IENZ_A_1640692_F0001_B.jpg

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