Amides Derived From Sclareolide as Cytotoxic Agents.

Authors

Júnio G Silva, Amanda S de Miranda, Tatiane F Borgati, Samuel M G Lopes, Sophie Hoenke, Juliana de Oliveira Silva, Fernanda F S Oliveira, André Luiz Branco de Barros, Adriano de Paula Sabino, René Csuk, Luiz C A Barbosa

Published in

Chemistry & biodiversity. Volume 23. Issue 7. Pages e71375.

Abstract

Natural products remain an invaluable source of inspiration for anticancer drug discovery. Herein, a series of 25 sclareolide (SC)-derived drimanamides was assessed for cytotoxicity against the A375, HT29, MCF-7, A2780, and HeLa tumor cell lines using the SRB assay. Structure-activity relationship analysis suggested that the introduction of aryl or triazolyl moieties was associated with increased potency relative to SC. Compounds 1 and 4 exhibited the most favorable cytotoxic profiles, with EC₅₀ values of 9.2 µM (HT29) and 11.9 µM (MCF-7) and a selectivity index (SI) of 3.3 and 2.5, respectively. Annexin V/PI assays indicated that both 1 and 4 increased apoptotic populations in MCF-7 cells, while cell cycle analysis showed modest accumulation in the G1 and G2 phases for derivative 1 and an increased S-phase population for 4. These findings highlight the drimane nucleus as a useful scaffold for anticancer agent design, revealing drimanamides as a novel cytotoxic class and 1 and 4 as promising candidates for further optimization.

PMID:
42455648
Bibliographic data and abstract were imported from PubMed on 16 Jul 2026.

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