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.
Highlights
Cancer is characterized by an uncontrolled growth of cells, which can spread to distant sites of the body with severe health consequences and is the second leading cause of death worldwide[1]
Compared to the previously recent published reviews[18], we focused this article on the carbazole derivatives exerting antitumour activity reported from 2012 to 2018, and we critically collected the most significant data
Many new cancer therapies have been developed in the last years, but this research field still presents many challenges
Summary
Cancer is characterized by an uncontrolled growth of cells, which can spread to distant sites of the body with severe health consequences and is the second leading cause of death worldwide[1]. Among the existing anti-cancer drugs, the carbazole scaffolds have been, for over half a century, the key structural motif of many biologically active compounds including natural and synthetic products[3]. Three derivatives have obtained marketing authorization with anti-cancer drug status in different countries. (Figure 1) and extracted from the leaves of Ochrosia elliptica (Apocynacae) before being entirely synthesized, could be considered as the first initial lead compound of carbazole analogues. The second derivative to obtain marketing authorization was alectinib bearing a 5H-benzo[b]carbazol-11(6H)-one scaffold (AF802, CH 5424802, RG7853, RO5424802, AlecensaVR ) (Figure 2).
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