Anticancer Acridones, Part 2—Acronycine-Type Derivatives Modified with 2,5-Dihydro-1,2,4-Triazine Moiety: Synthesis and In Vitro Evaluation
Andrey A. Zonov, Ramil F. Fatykhov, Igor A. Khalymbadzha, Ainur D. Sharapov, Anastasia P. Potapova, Ilya I. Butorin, Vsevolod V. Melekhin, Anastasia V. Paramonova, Emiliya V. Nosova
TL;DR
Researchers synthesized new anticancer compounds based on acridone and found they are effective against certain cancer cells.
Contribution
Novel noracronycine derivatives with 1,2,4-triazine show enhanced anticancer activity and selectivity.
Findings
Eight new noracronycine derivatives with 1,2,4-triazine were synthesized and tested.
Compounds showed micromolar activity and selectivity for glioblastoma and breast cancer cells.
Adding a pyridyl group to the triazine core increased cytotoxicity toward cancer cells.
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.
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Taxonomy
TopicsSynthesis and Characterization of Heterocyclic Compounds · Synthesis and bioactivity of alkaloids · Cancer therapeutics and mechanisms