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Benzosuberone is a promising scaffold with a remarkably varied pharmacological profile that has been attracting significant interest in the potential development of anticancer agents. This review focuses on the historical interest, diversity of chemical structures, and different medicinal applications of benzosuberone derivatives, particularly as agents with potential anticancer activity. We investigated the relationship between structure modification and biological activity by focusing on the molecular hybrids of the present hit with various functionalities or heterocycles, which led to improved cytotoxicity against several cancer cell lines, and miscellaneous biological activities such as antimicrobial, antiviral, neurological, antiparasitic, anti‐diabetic, and antitubercular activities. Detailed in vitro analyses showed promising cytotoxicity against breast, lung, and colon cancers, presenting IC 50 values in the low micromolar and submicromolar ranges and low toxicity profiles concerning normal cells. Novel approaches, including the hybrid molecule, combinatory therapy, and nano‐formulation, are suggested to go beyond the current obstacles and expand the applications of benzosuberone‐based derivatives toward clinical applications. This combined study demonstrates that the benzosuberone scaffold is a privileged structure in the search for miscellaneous biological drugs with high therapeutic potential.
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Nafie et al. (2026) studied this question.
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