Work

Development of 1,2,3‐Triazolopyridazinone Derivatives as Potential Caspase 3 and Apoptosis Inducers: Design, Synthesis and Anticancer Activity Studies

Year: 2025

Type: article

Abstract: Herein, the synthesis, anticancer activity and apoptotic pathways of 1,2,3-triazolopyridazinones compounds, which are similar to DNA bases not previously found in the literature have been investigated. To achieve this goal, it is designed the hybrid molecules combining triazole and pyridazinone/pyridazithione structures, bearing a lipophilic group (benzyl/phenyl) at the one position and benzene with electron withdrawing or donating groups at five positions, with high pharmacophoric properties on the same scaffold structure. The representative compounds in this series 5a, 5c, 6a and 8c exhibited higher anticancer activity than other compounds and cisplatin control against breast (MCF-7) and lung (A549) cell lines. These compounds were less toxic when tested against the noncancerous L929 cell line. In addition, the apoptotic effect mechanisms of these compounds were confirmed by AO/EB staining and caspase 3 activity results. These findings indicate that some derivatives of these compounds could be effective therapeutic agents for the treatment of cancer disease with an apoptosis-promoting.

Source: Journal of Biochemical and Molecular Toxicology

DOI: 10.1002/jbt.70216

Authors: Guler Yagiz Erdemir, Ali Kuruçay, Burhan Ates, Aliye Altundas

Institutions: Gazi University, Inonu University

Language: English

Topic: Synthesis and biological activity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,020