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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 and Radical Scavenging Properties of Selenophenyl Benzamide Anologs
    (Gazi Univ, 2016) Doganay, Kadir; Karaaslan, Merve Goksin; Ates, Burhan; Altundas, Aliye
    Free radicals that result from different kinds of oxidative stress have been concerned in a variety of human disorders, from cardiac ischemia to those affecting the central nervous system. So, there is an increasing interest in the development of antioxidant molecules that can protect cells against free radical damages. Sets of tetrasubstituted selenophene amides 4a-e were synthesized by reaction of 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b] selenophen-3-carbonitrile (2) with benzoyl chloride derivatives and the structures of the amide derivatives were characterized by MS, H-1-NMR, C-13-NMR and IR spectra. The synthesized compounds (4a-e) were evaluated in terms of in vitro. The antioxidant properties were determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging properties and IC50 values of the compounds were in the range from 3.794 to 5.644 mg/mL. Compounds 4c and 4e showed predominant radical scavenging activity among the synthesized analogues.
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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.
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    Synthesis, inhibition properties against xanthine oxidase and molecular docking studies of dimethyl N-benzyl-1H-1,2,3-triazole-4,5-dicarboxylate and (N-benzyl-1H-1,2,3-triazole-4,5-diyl)dimethanol derivatives
    (Academic Press Inc Elsevier Science, 2021) Yagiz, Guler; Noma, Samir Abbas Ali; Altundas, Aliye; Al-khafaji, Khattab; Taskin-Tok, Tugba; Ates, Burhan
    This study focused on synthesis various dimethyl N-benzyl-1H-1,2,3-triazole-4,5-dicarboxylate and (N-benzyl-1H-1,2,3-triazole-4,5-diyl)dimethanol derivatives under the conditions of green chemistry without the use of solvent and catalysts. Their inhibition properties were also investigated on xanthine oxidase (XO) activity. All dimethanol and dicarboxylate derivatives exhibited significant inhibition activities with IC50 values ranging from 0.71 to 2.25 mu M. Especially, (1-(3-bromobenzyl)-1H-1,2,3-triazole-4,5-diyl)dimethanol (5c) and dimethyl 1-(4-chlorobenzyl)-1H-1,2,3-triazole-4,5-dicarboxylate (6 g) compounds were found to be the most promising derivatives on the XO enzyme inhibition with IC50 values 0.71 and 0.73 mu M, respectively. Moreover, the double docking procedure was to evaluate compound modes of inhibition and their interactions with the protein (XO) at atomic level. Surprisingly, the docking results showed a good correlation with IC50 [correlation coefficient (R-2 = 0.7455)]. Also, the docking results exhibited that the 5c, 6f and 6 g have lowest docking scores -4.790,-4.755, and -4.730, respectively. These data were in agreement with the IC50 values. These results give promising beginning stages to assist in the improvement of novel and powerful inhibitor against XO.
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    Synthesis, reaction, and evaluation of the anticancer activity of 6,7,8,9-tetrahydro-5H-cyclohepta[4,5]selenopheno[2,3-d]pyrimidine derivatives
    (Tubitak Scientific & Technological Research Council Turkey, 2016) Doganay, Kadir; Kelestemur, Unzile; Balcioglu, Sevgi; Ates, Burhan; Altundas, Aliye
    The cyclocondensation of 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]selenophene-3-carbonitrile (1) with formic acid and formamide gave the selenophenopyrimidine 15 and selenophenopyrimidone 6 derivatives. The reaction of 6 with phosphorus oxychloride produced 4-chloro-6,7,8,9-tetrahydro-5H-cyclohepta[4,5] seleno[2,3-d]pyrimidine (12), the key compound for our nucleophilic substitution reactions. The hydrazinoselenophenopyrimidine 19 obtained from the reaction of 12 with hydrazine hydrate was converted to its tetrazoloselenophenopyrimidine 21 and triazoloselenophenopyrimidine 26 derivatives. Moreover, the chloropyrimidine derivative was reacted with pyrrolidine and morpholine to afford 4-(1-pyrrolidinyl)-6,7,8,9-tetrahydro-5H-cylohepta[4,5]selenopheno [2, 3-d]pyrimidine (27) and 4- (6,7,8,9-tetrahydro-5H-cyclohept a [4,5]selenopheno [2,3-d]pirimidin-4-yl)morpholine (28). Anticancer activities of the synthesized compounds were investigated against the MCF-7 breast cancer cell line and the IC50 values of these compounds were in the range of 70.86-250.06 mu M.