Synthesis, antioxidant, and antiproliferative activity of apocynin triazole derivatives containing 3,4-difluorophenyl-cyclopropanamine motif.

Authors

Maria Carolina Theisen, Bianca Costa Maia-do-Amaral, Isis Apolo Silveira de Borba, Andressa Motta Castro, Jamile Buligon Peripolli, Daniele Rubert Nogueira-Librelotto, Fernando Fumagalli

Published in

Natural product research. Pages 1-7. Jul 07, 2026. Epub Jul 07, 2026.

Abstract

Apocynin is a natural product known for its antioxidant activity and potential medicinal applications. However, it is still unexplored in semisynthetic strategies. Considering the need for the development of new therapeutic alternatives for cancer treatment, this work explored the reactivity of apocynin towards the synthesis of potential triazole-based antineoplastic compounds inspired by histone lysine demethylase-specific 1 (LSD1) inhibitors and minor groove binders and evaluated their cytotoxic activity in the breast cancer cell line Michigan Cancer Foundation-7 (MCF-7) and antioxidant activity, comparing them to bromine analogues. As a result, apocynin derivative 7b showed promising growth inhibition (GI₅₀ = 15.5 µM) and low antioxidant activity. The cell cycle analysis showed increased cell arrest in the G1 phase, corroborating potential inhibition of LSD1. This work provided new insights into the synthetic use of apocynin and identified an interesting compound for further studies.

PMID:
42412982
Bibliographic data and abstract were imported from PubMed on 08 Jul 2026.

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