1,2,3-Triazole-Linked Chalcones as Privileged Scaffolds in Anticancer Agents
Archiv der Pharmazie, cilt.359, sa.6, 2026 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 359 Sayı: 6
- Basım Tarihi: 2026
- Doi Numarası: 10.1002/ardp.70291
- Dergi Adı: Archiv der Pharmazie
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, Chemical Abstracts Core, Chimica, EMBASE, MEDLINE, Health Research Premium Collection (ProQuest), Pharma Collection (ProQuest)
- Anahtar Kelimeler: 1,2,3-triazolediester, A549, CaCo-2, cancer, chalcones, cytotoxicity
- Gazi Üniversitesi Adresli: Evet
Özet
A new series of extended-functionality triazole-substituted chalcone derivatives was synthesized, and their in vitro anti-proliferative and cytotoxic profiles were evaluated using cancer and non-cancer cell models. First, all compounds were screened in the FaDu head and neck squamous cell carcinoma cell line to identify the most active candidates with comparatively lower IC50 values. Compounds 6c, 6e, and 6f reduced FaDu cell viability to 42.62 ± 12.21%, 34.49 ± 4.99%, and 31.13 ± 4.76% of control, respectively. These three compounds also decreased viability of CaCo-2 human colon cancer cells and A549 human lung adenocarcinoma cells, showing micromolar-range activity (IC50 < 50 µM) across cancer cell lines of different origins. To obtain a preliminary indication of selectivity, we additionally tested a non-cancer, immortalized prostate epithelial cell line (PNT1a). In this model, 6c/6e/6f displayed relatively lower cytotoxicity than in cancer cells, suggesting a preliminary selectivity window within the tested assay framework. Among them, 6f the most active compound in our series—significantly reduced colony formation, comparable to paclitaxel. In apoptosis-related assessments, 6f increased apoptosis-associated readouts in cancer cells relative to control, although further confirmation is needed with additional orthogonal assays. Overall, our results identify 6c, 6e, and especially 6f as moderately active lead compounds for further optimization of triazole-chalcone hybrids and support continued structure–activity-guided development to improve potency and selectivity.