Anticancer Acridones, Part 2—Acronycine-Type Derivatives Modified with 2,5-Dihydro-1,2,4-Triazine Moiety: Synthesis and In Vitro Evaluation

International Journal of Molecular Sciences 2026 Open access

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Authors: Andrey A. Zonov, Ramil F. Fatykhov, Igor А. Khalymbadzha, Ainur D. Sharapov, Anastasia P. Potapova, Ilya I. Butorin, Vsevolod V. Melekhin, A. M. Paramonova, Emiliya V. Nosova
DOI: 10.3390/ijms27041969
Cited by: 1
References: 36

Abstract

This manuscript presents the synthesis of eight novel noracronycine derivatives containing 1,2,4-triazine moiety and evaluates their anticancer activity in vitro. The obtained compounds exhibit activity in the micromolar range and show selectivity towards glioblastoma A172 and breast cancer Hs578T cells. Compounds incorporating a dihydrotriazine moiety demonstrate an enhanced anticancer profile when compared to a noracronycine derivative lacking a triazine substituent. Furthermore, introducing a pyridyl group into the triazine core increases selective cytotoxicity toward cancerous cells. The lead compound exhibits an IC50 value of 3.4 μM for glioblastoma A172, with a selectivity index of 7.59. Mechanistic studies reveal that the obtained compounds slow down cell division, while no significant apoptosis was detected.

Fields of Study & Subjects

Synthesis and Characterization of Heterocyclic Compounds Synthesis and bioactivity of alkaloids Cancer therapeutics and mechanisms

Publication details

Journal / source
International Journal of Molecular Sciences
Publisher
MDPI AG
Volume
27
Issue
4
Pages
1969–1969
Publication date
18 February 2026
Language
EN