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Benzophenanthridine alkaloids are a class of isoquinoline compounds, which are widely found in the plants of papaveraceae, corydalis, and rutaceae. Biological activities and clinical studies have shown that benzophenanthridine alkaloids have inhibitory effects on many cancers. Considering that the anticancer activities and mechanisms of many natural benzophenanthridine alkaloids have been discovered in succession, the purpose of this paper is to review the anticancer effects of benzophenanthridine alkaloids and explore the application potential of these natural products in the development of antitumor drugs. A literature survey was carried out using Scopus, Pubmed, Reaxys, and Google Scholar databases. This review summarizes and analyzes the current status of research on the antitumor activity and antitumor mechanism of natural products of benzophenanthridine from different sources. The research progress of the antitumor activity of natural products of benzophenanthridine from 1983 to 2023 was reviewed. The antitumor activities of 90 natural products of benzophenanthridine and their related analogues were summarized, and the results directly or indirectly showed that natural products of benzophenanthridine had the effects of antidrug-resistant tumor cell lines, antitumor stem cells, and inducing ferroptosis. In conclusion, benzophenanthridine alkaloids have inhibitory effects on a variety of cancers and have the potential to counteract tumor resistance, and they have great application potential in the development of antitumor drugs. [ABSTRACT FROM AUTHOR]

Currently, the number of new cancer cases and deaths worldwide is increasing year on year. In addition to the requirement for cancer prevention, the top priority is still to seek the effective cure of cancer. In over a half century of constant exploration, increasing attention has been paid to the excellent anticancer activity of natural products, with more and more natural products isolated, identified and detected. For this study, the focus lies the natural products of bisindole, where two indole molecules are indirectly linked or directly polymerized, developing the diversity of structure and mechanism, accompanied with the better anticancer activity than monomers. There has been a long history of applying indirubin and vincristine in cancer treatment, verifying the anticancer effect of bisindoles. Vincribine, midostaurin and other anticancer drugs have also been developed and commercialized. In this paper, a review regarding the potential therapeutic effect of bisindole alkaloids extracted from various natural products was carried out, in which the progress made in research of 242 bisindole alkaloids for cancer treatment was introduced. These compounds may be applicable as medicinal products for clinical research in the future. [Display omitted] • 242 bisindole natural products showed different degrees of anticancer activity. • The dimeric indole structure acts as the crux to bisindoles. • Bisindoles provide a variety of leading structures for novel anticancer drugs. [ABSTRACT FROM AUTHOR]