Person: TÜRE, ASLI
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TÜRE
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ASLI
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Publication Metadata only Novel fluoroquinolones containing 2-arylamino-2-oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies(WILEY, 2022) TÜRE, ASLI; Kulabas, Necla; Ture, Asli; Bozdeveci, Arif; Krishna, Vagolu Siva; Karaoglu, Sengul Alpay; Sriram, Dharmarajan; Kucukguzel, IlkayNovel substituted fluoroquinolone derivatives, compounds 6-20 were designed, synthesized, and evaluated for antituberculosis and antibacterial activity. Antibacterial activities of the compounds were determined and compound 14 was found to be the most potent antimicrobial agent owing to minimal inhibitory concentration (MIC) value of <1.16 mu g/mu l for all tested bacteria. Further, compounds were tested in vitro for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Most of the compounds showed antimycobacterial effects with 1.56-25.00 mu g/ml MIC values. Compounds 14 and 18 were found to be the most active derivatives due to their MIC at 1.56 mu g/ml. Selected compounds 11, 14, 17, and 18 were tested for M. tuberculosis DNA supercoiling assay and they had IC50 values within a range of 6.35-15 mu M. Mechanism of binding to DNA gyrase enzymes was evaluated using in silico molecular modeling studies and it was shown that compounds 6-20 adopt a similar binding mode as already known for fluoroquinolone drugs.Publication Open Access Design and synthesis of new heterocyclic compounds containing 5-[(1H-1,2,4-triazol-1-yl)methyl]-3H-1,2,4-triazole-3-thione structure as potent hEGFR inhibitors(2023-01-01) TÜRE, ASLI; KOLCUOĞLU Y., BEKİRCAN O., Fazli H., Sahin E., TÜRE A., AKDEMİR A., Hamarat Sanlier S.© 2023 Informa UK Limited, trading as Taylor & Francis Group.EGFR is one of the important mediators of the signaling cascade that determines key roles in various biological processes such as growth, differentiation, metabolism and apoptosis in the cell in response to external and internal stimuli. In recent years, it has been proven that although this enzyme activity is tightly regulated in normal cells, if the enzyme activity cannot be controlled, it can lead to malignancy. EGFR is also considered a prominent macromolecule in targeted cancer chemotherapy. For this purpose, a comprehensive modeling studies were conducted against EGFR protein and novel molecules containing 5-[(1H-1,2,4-triazol-1-yl)methyl]-3H-1,2,4-triazole-3-thione structure were suggested to be synthesized. Among the synthesized molecules, compounds 7c, 8c, 8f and 8g were determined to have significant IC50 values. Compound 8g was found to have the IC50 value closest to the very well-known EGFR inhibitor Gefitinib with its noncompetitive inhibition form. K i value of compound 8g was calculated as 0.00232 µM. Communicated by Ramaswamy H. Sarma.Publication Metadata only Synthesis, computational molecular docking analysis and effectiveness on tyrosinase inhibition of kojic acid derivatives(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) TÜRE, ASLI; Karakaya, Gulsah; Ture, Asli; Ercan, Ayse; Oncul, Selin; Aytemir, Mutlu DilsizTyrosinase inhibitors have become increasingly important as whitening agents and for the treatment of pigmentary disorders. In this study, the synthesis of kojic acid derivatives having 2-substituted-3-hydroxy-6-hyroxymethyl/chloromethyl/methyl/morpholinomethylpiperidinyl- methyl/pyrrolidinylmethyl-4H-pyran-4-one structure (compounds 1-30) with inhibitory effects on tyrosinase enzyme were described. One-pot Mannich reaction was carried out by using kojic acid/chlorokojic acid/allomaltol and substituted benzylpiperazine derivatives in presence of formaline. Subsequently, cyclic amine (morpholine, piperidine and pyrrolidine) derivatives of the 6th-position of chlorokojic acid were obtained with nucleophilic substitutions in basic medium. The structures of new compounds were identified by FT-IR, H-1- and C-13 NMR, ESI-MS and elemental analysis data. The potential mushroom tyrosinase inhibitory activity of the compounds were evaluated by the spectrophotometric method using L-DOPA as a substrate and kojic acid as the control agent. The potential inhibitory activity was also investigated in silico using molecular docking simulation method. Tyrosinase inhibitory action was significantly more efficacious for several compounds (IC50: 86.2-362.1 mu M) than kojic acid (IC50: 418.2). Compound 3 bearing 3,4-dichlorobenzyl piperazine moiety was proven to have the highest inhibitory activity. The results of docking studies showed that according to the predicted conformation of compound 3 in the enzyme binding site, hydroxymethyl group provides a metal complex with copper ions and enzyme. Thus, this interaction explain the high inhibitory activities of the compounds 1, 3 and 4 possessing hydroxymethyl substituent supporting the mushroom assay results with docking studies. In accordance with the results, it is suggested that Mannich bases of kojic acid bearing substituted benzyl piperazine groups (compounds 1, 3, 4, 11, 13, 14, 23, 24, 28, and 29) could be promising antityrosinase agents. Additionally, considering the relationship between tyrosinase inhibitory activity results and molecular docking, a new tyrosinase inhibition mechanism can be proposed.Publication Metadata only Molecular modeling and assessment of cytotoxic and apoptotic potentials of imatinib analogues featuring (thio)urea motifs in human leukemia and lymphoma cells(MARMARA UNIV, 2020) TÜRE, ASLI; Bingol Ozakpinar, Ozlem; Ture, Asli; Kucukguzel, IlkayImatinib is a well-known anticancer drug. In this study, cytotoxic properties of thirty-two imatinib analogues featuring (thio)urea motifs have been evaluated against chronic myeloid leukemia (K562), Burkitt lymphoma (Raji) and mouse embryonic fibroblast (NIH 3T3) cells. IC50 values of selected eleven compounds were calculated against K562 and NIH 3T3 cells. Apoptotic properties of the most active three compounds were evaluated on K652 cells subsequently. Favorably, compounds 19, 31 and 32 induced early apoptotic changes on K562 cells. Loss of membrane potential as well as caspase-3 and caspase-9 activation was determined in the present study. Levels of anti-apoptotic proteins, Bcl-XL and Bcl-2 decreased after the implementation of compounds 19, 31 and 32 at 10 mu M and 50 mu M concentrations. To reveal further molecular insight into the anticancer activity of the compounds, compounds 19, 31 and 32 were docked into ABL kinase protein as imatinib shows anticancer activity by inhibiting this enzyme. Modeling studies demonstrated significant molecular interactions between compounds 19, 31 and 32 and ABL protein. Compounds 19, 31 and 32 showed excellent superposition with imatinib in the binding site of ABL. These findings suggest that compounds 19, 31 and 32 have potential to show anticancer activity against chronic myeloid leukemia.Publication Open Access Synthesis and molecular modeling of some novel hydroxypyrone derivatives as antidermatophytic agents(2022-10-01) TÜRE, ASLI; Karakaya G., Ozdemir A., Ture A., ÖZÇELİK B., Aytemir M.Dermatophytes are pathogenic fungi, comprising the major cause of superficial fungal infections called dermatophytes. Although they infect keratinized tissues such as skin, nail, and hair, invasive serious infections may occur in immunocompromised patients. However, current antifungal drugs show considerable drawbacks, such as toxicity and multiple drug resistance, compelling and directing researches for new antidermatophyte agents. Herein, a series of hydroxypyrone bearing compounds inspired from the natural metabolite kojic acid was reported. Their antidermatophytic effects of the compounds against Microsporum gypseum, Trichophyton mentagrophytes var. erinaceid, and Epidermophyton floccosum were evaluated. The cytotoxicity of the compounds on healthy (MRC-5) and carcinogenic (He-La) cell lines was also investigated, and their cytopathogenic effects were expressed as maximum non-toxic concentrations. According to the activity studies, compounds 10 and 22 were found as the most promising antidermatophytic agents (MIC: 2 mu g/ml), exhibiting comparable effect with that of griseofulvin (MIC: 0.5-1 mu g/ml) and terbinafine (MIC: 0.125-0.5 mu g/ml) which are the most widely used agents for treating mycoses caused by dermatophytes. Molecular docking analysis of the most active compounds, compound 10 and compound 22, with homology model of beta-tubulin protein was carried out to investigate the possible binding conformation of the compounds in the targeted macromolecule.Publication Metadata only Synthesis and evaluation of novel 1,3,4-thiadiazole-fluoroquinolone hybrids as antibacterial, antituberculosis, and anticancer agents(SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2018) TÜRE, ASLI; Demirci, Asli; Karayel, Kaan Gokce; Tatar, Esra; Oktem Okullu, Sinem; Unubol, Nihan; Tasli, Pakize Neslihan; Kocagoz, Zuhtu Tanil; Sahin, Fikrettin; Kucukguzel, IlkayA series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16-25 were synthesized by reacting the corresponding N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-chloroacetamides with ciprofloxacin or norfloxacin. The purity and identity of the synthesized compounds were determined by the use of chromatographic and spectral techniques (NMR, IR, MS, etc.) besides elemental analysis. Antibacterial, antituberculosis, and anticancer activity of the target compounds were evaluated against selected strains and cancer cell lines. Compound 20 was appreciated as the most active agent representing antibacterial activity against Escherichia coli and Staphylococcus aureus with MIC values of 4 mu g/mL and 2 mu g/mL, respectively. Amongst the synthesized fluoroquinolone derivatives, compounds 19 and 20 were found to have modest antitubercular activity with 8 mu g/mL MIC values for each. Most potent derivative, compound 20 was docked against Staphylococcus aureus and Mycobacterium tuberculosis DNA gyrase enzymes to visualize the possible conformation of the compound. Additionally, anticancer activities of target compounds were evaluated on seven different cancer cell lines.Publication Metadata only Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) TÜRE, ASLI; Ture, Asli; Kulabas, Necla; Dingis, Serap Ipek; Birgul, Kaan; Bozdeveci, Arif; Karaoglu, Sengul Alpay; Krishna, Vagolu Siva; Sriram, Dharmarajan; Kucukguzel, IlkayTwenty-one novel alkyl/acyl/sulfonyl substituted fluoroquinolone derivatives were designed, synthesized and evaluated for their anti-tuberculosis and antibacterial activity. The targeted compounds were synthesized by the introduction of alkyl, acyl or sulfonyl moieties to the basic secondary amine moiety of moxifloxacin. Structures of the compounds were enlightened by FT-IR, H-1 NMR, C-13 NMR and HRMS data besides elemental analysis. Compounds were initially tested in vitro for their anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv using microplate alamar blue assay. Minimal inhibitory concentration (MIC) values of all compounds were found between > 25.00-0.39 mu g/mL while compounds 1, 2 and 13 revealed an outstanding activity against M. tuberculosis H37Rv with MIC values of 0.39 mu g/mL. Activities of compounds 1-21 against to a number of Gram-positive and Gram-negative bacteria and fast growing mycobacterium strain were also investigated by agar well diffusion and microdilution methods. According to antimicrobial activity results, compound 13 was found the most potent derivative with a IC50 value of < 1.23 mu g/mL against Staphylococcus aureus and clinical strain of methicillin-resistant clinical strain of S. aureus.Publication Metadata only Novel 2,6-disubstituted pyridine hydrazones: Synthesis, anticancer activity, docking studies and effects on caspase-3-mediated apoptosis(ELSEVIER, 2021) TÜRE, ASLI; Senkardes, Sevil; Ture, Asli; Ekrek, Sedanur; Durak, Asim Tugrul; Abbak, Muruvvet; Cevik, Ozge; Kaskatepe, Banu; Kucukguzel, Ilkay; Kucukguzel, S. GunizNovel pyridine-based dihydrazones (3a-l) were synthesized by the condensation of appropriate aldehydes and pyridine-2,6-dicarbohydrazide (2) which was obtained by the treatment of dimethyl pyridine-2,6-dicarboxylate (1) with hydrazine hydrate. Structures of all the synthesized compounds were supported by their FTIR, H-1 NMR, C-13 NMR and microanalytical data. The compounds were screened primarily for their antibacterial activities as well as anticancer activities. None of the synthesized compounds had important antibacterial activity. Among the compounds which were tested against human colon cancer cell line (HT-29), compounds 3f and 3k showed significant activity (IC50=6.78 mu M for compound 3f, IC50 = 8.88 mu M for compound 3k). In addition, compound 3g exhibited promising activity against Ishikawa human endometrial cancer cell line (ISH) with an IC50 value of 8.26 mu M. At 10 mu M, compounds 3f, 3k and 3g caused morphological changes of HT-29 and ISH cells and caspase-3 activation. In addition, these compounds were evaluated against NIH 3T3 mouse embriyonic fibroblast cell line and all synthesized compounds (3a-l) were found to be less toxic than paclitaxel. Moreover, possible inhibition mechanism of compound 3g was evaluated in silico against BRAF kinase enzyme. (C) 2020 Elsevier B.V. All rights reserved.Publication Metadata only Synthesis, anticancer activity, toxicity evaluation and molecular docking studies of novel phenylaminopyrimidine-(thio)urea hybrids as potential kinase inhibitors(ELSEVIER SCI LTD, 2019) TÜRE, ASLI; Ture, Asli; Kahraman, Deniz Cansen; Cetin-Atalay, Rengul; Helvacioglu, Sinem; Charehsaz, Mohammad; Kucukguzel, IlkayThirty-two novel urea/thiourea compounds as potential kinase inhibitor were designed, synthesized and evaluated for their cytotoxic activity on breast (MCF7), colon (HCT116) and liver (Huh7) cancer cell lines. Compounds 10, 19 and 30 possessing anticancer activity with IC50 values of 0.9, 0.8 and 1.6 mu M respectively on Huh7 cells were selected for further studies. These hit compounds were tested against liver carcinoma panel. Real time cell electronic sensing assay was used to evaluate the effects of the compounds 10, 19 and 30 on the growth pattern of liver cancer cells. Apoptotic cell death and cell cycle analysis upon treatment of liver carcinoma cells with hit compounds were determined. A significant apoptotic cell death was detected upon treatment of Huh7 and Mahlavu cells with compound 30 after 48 h of treatment. Additionally, compound 10 caused cell cycle arrest at G0/G1 phase. Mutagenicity of hit compounds was evaluated. Assertively, these compounds were not found to be mutagenic on Salmonella typhimurium strains TA98 and TA100. To understand the binding modes of the synthesized compounds, molecular docking studies were performed using the crystal data of VEGFR and Src-kinase enzymes in correlation with anticancer activities.Publication Metadata only Design, synthesis, and anticancer activity of novel 4-thiazolidinone-phenylaminopyrimidine hybrids(SPRINGER, 2021) TÜRE, ASLI; Ture, Asli; Ergul, Mustafa; Ergul, Merve; Altun, Ahmet; Kucukguzel, Ilkay4-Thiazolidinones and phenylaminopyrimidines are known as anticancer agents. Imatinib is the pioneer phenylaminopyrimidine derivative kinase inhibitor, which is used for the treatment of chronic myeloid leukemia. With a hybrid approach, a novel series of 5-benzylidene-2-arylimino-4-thiazolidinone derivatives containing phenylaminopyrimidine core were designed, synthesized, and tested for their anticancer activity on K562 (chronic myeloid leukemia), PC3 (prostat cancer), and SHSY-5Y (neuroblastoma) cells. Since superior anticancer activity was observed on K562 cells, further biological studies of selected compounds (8, 15, and 34) were performed on K562 cells. For the synthesis of designed compounds, thiourea compounds were converted to 2-imino-1,3-thiazolidin-4-ones with alpha-chloroacetic acid in the presence of sodium acetate. 5-Benzylidene-2-imino-1,3-thiazolidin-4-one derivatives were obtained by Knoevenagel condensation of 2-imino-1,3-thiazolidin-4-ones with related aldehydes. Compounds 8, 15, and 34 were evaluated for cell viability, apoptosis studies, cell cycle experiments, and DNA damage assays. IC50 values of compounds 8, 15, and 34 were found as 5.26 +/- 1.03, 3.52 +/- 0.91, and 8.16 +/- 1.27 mu M, respectively, in K562 cells. Preferably, these compounds showed less toxicity towards L929 cells compared to imatinib. Furthermore, compounds 8 and 15 significantly induced early and late apoptosis in a time-dependent manner. Compounds 15 and 34 induced cell cycle arrest at G0/G1 phase and compound 8 caused cell cycle arrest at G2/M phase. Based on DNA damage assay, compounds 8 and 15 were found to be more genotoxic than imatinib towards K562 cells. To put more molecular insight, possible Abl inhibition mechanisms of most active compounds were predicted by molecular docking studies. In conclusion, a novel series of 5-benzylidene-2-arylimino-4-thiazolidinone derivatives and their promising anticancer activities were reported herein. [GRAPHICS] .