ReviewMolecules (Basel, Switzerland)2026
Tetrahydrocarbazole as a Versatile Scaffold in Drug Discovery: A Cross-Target SAR Analysis and Design Paradigms.
Review in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Authors and funding
10 authors.
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Abstract
Tetrahydrocarbazole (THCz) is a privileged scaffold validated by clinically approved drugs such as ondansetron, frovatriptan, and ramatroban and exhibits diverse bioactivities including antimicrobial, antitumor, antidiabetic, and neuroprotective effects. Despite extensive structure-activity relationship (SAR) studies, a systematic integration of findings across different therapeutic targets has been lacking. This review provides a comprehensive SAR dissection of THCz derivatives across key targets (bacterial sliding clamp, BTK, HDAC, AMPK, etc.), analyzing how modifications at key positions of the core scaffold (N-9, C-1, and C-6) influence potency and selectivity. Notably, we highlight four emerging design paradigms: pharmacophore hybridization, conformational constraint, cross-target SAR decoding, and precision intervention. By consolidating fragmented knowledge into a practical cross-target SAR matrix, this review offers a strategic framework for the rational design of next-generation THCz-based therapeutics.
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