Recent research progress of β-carbolines as privileged scaffold in the discovery of anticancer agent (2019-2024).

Bioorg Med Chem

School of Health and Life Sciences, University of Health and Rehabilitation Sciences, Qingdao 266001, China; School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China. Electronic address:

Published: November 2025


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Article Abstract

Cancer remains a formidable global health challenge, driving the need for targeted therapeutic agents to improve clinical outcomes. Natural and synthetic β-carboline alkaloids, characterized by their indole-based heterocyclic structures, have emerged as privileged scaffolds in oncology drug development due to their multimodal antitumor mechanisms. This review systematically evaluates recent advancements in β-carboline derivatives research, with emphasis on structural modification strategies, structure-activity relationships, and mechanistic elucidation of tumor suppression pathways. Through multidimensional evaluation and analysis, we propose actionable directions for the development of β-carboline derivatives with enhanced pharmacological profiles for treating various cancers.

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http://dx.doi.org/10.1016/j.bmc.2025.118325DOI Listing

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