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    Development of 1,2,3-Triazolopyridazinone Derivatives as Potential Caspase 3 and Apoptosis Inducers: Design, Synthesis and Anticancer Activity Studies
    (Wiley, 2025) Erdemir, Guler Yagiz; Kurucay, Ali; Ates, Burhan; Altundas, Aliye
    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.
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    Novel 1,2,3-triazole-benzimidazole hybrid structures acting as promising anticancer agents against breast and colon cancer cell
    (Springer Wien, 2025) Erdemir, Guler Yagiz; Gunduz, Nermin; Ates, Burhan; Altundas, Aliye
    In this paper, a series of new 1,2,3-triazole-benzimidazoles hybrid structures, may exhibit potent anticancer activities, were designed and synthesized. The synthesis of the 1,2,3-triazole-benzimidazoles began with the preparation of 1,2,3-triazoles containing formyl precursors and then reacted with o-phenylenediamine to give 1,2,3-triazole-benzimidazole hybrid structures. 1,2,3-Triazole-benzimidazole complexes were tested for in vitro inhibition against human cancer cell lines such as breast (MCF-7) and colon (HCT116) by MTT assay. In particular, methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate and methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(2-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate showed the best activity in the MCF-7 line with IC50 values of 52.15 and 42.96 mu g/cm3, respectively. For the HCT116 line, methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate and methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(4-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate showed the highest activity with IC50 values of 15.89 mu g/cm3 and 18.89 mu g/cm3, respectively. In summary, the results of this study show that methyl 5-(1H-benzo-[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate with further modifications could serve as a leading drug candidate in future cancer studies in both MCF-7 and HCT116 strains.
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    Synthesis of 1,4-disubstituted-1,2,3-Triazole derivatives for investigation of inhibition and molecular docking studies against Xanthine Oxidase
    (Scienceın Publications, 2023) Mirdan, Mustafa Nabeel Mirdan; Erdemir, Guler Yagiz; Noma, Samir Abbas Ali; Tok, Tugba Taskin; Ates, Burhan; Altundas, Aliye
    This study evaluates the inhibition effect of new 1,4-disubstituted-1,2,3-triazoles against Xanthine Oxidase supplemented by molecular modelling. Nine compounds of 1,4-disubstituted-1,2,3-triazoles by Sharpless's approach have been synthesized in this report. The structures of the synthesized compounds were characterized using FT-IR, H-1 and C-13-NMR and Mass spectroscopies Among these synthesized molecules (5bromothiophen-2-yl)(1-(3-fluorobenzyl)-1H-1,2,3-triazole-4-yl)methanone (9f) and (5-Bromothiophen-2-yl(1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-yl)methanone (9h) showed better activity against Xanthine oxidase (XO) compared to allopurinol. In the light of the XO inhibition results, triazoles having of ketone moiety (9f-i) were found to be more active than triazoles of ketone-free (9a-e). These results were supported by docking models. The docking calculations of the target XO with nine available compounds showed good binding energies with favourable binding interactions. These findings were particularly evident that 9f (BE -7.29 kcal/mol) and 9h (BE -7.59 kcal/mol) are represented encouraging higher inhibition properties towards xanthine oxidase (XO), compared to allopurinol as a reference compound. Significant binding energies and interactions obtained by performing the docking studies are demonstrated, in particular, that the compounds 9f and 9h may be more potential bio compounds than the positive compounds, allopurinol, and febuxostat.