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    Activity of bisbenzimidazoles derivatives to Staphylococcus epidermidis
    (Chemical Publishing Co., 2007) Algul, Oztekin; Duran, Nizami
    Biomaterial-associated infections, most frequently caused by Staphylococcus epidermidis and Staphylococcus aureus, are of increasing importance in modern medicine. The most important factor in the pathogenesis of biomaterial- associated staphylococcal infections is the formation of adherent, multilayered bacterial biofilms. The aim of this study was to synthesize bis(benzimidazole) derivatives and evaluate their in vitro antimicrobial activity against the growth of gram positive (Enterococcus faecalis, methicillin resistant S. aureus, methicillin sensitive S.aureus, S. epidermidis and S. epidermidis RP12 (slime producing), gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and pathogenic fungi (Candida albicans, Candida krusei, Candida parapsilosis, Candida tropicalis and Candida glabrata). The antimicrobial activity of bis(benzimidazole) derivatives was higher in gram positive bacteria. Bis(benzimidazole) derivatives were inhibited gram positive bacteria at the concentration range of 12.5-100 ?g/mL. All compounds were shown to be bacteriostatic as well as bacteriocidal for cultures of S. aureus and S. epidermidis strains, regardless of their antibiotic susceptibility profile. This was demonstrated by using simultaneously the optical density measuring method and 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide-reduction assay. The highest activity was shown by 1,2-di(1H-benzo[d]imidazol-2-yl)ethane which demonstrated interesting activity regarding its effect on 24 h old staphylococcal biofilm cells viability.
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    Bisbenzoxazole Derivatives: Design, Synthesis, in Vitro Antimicrobial, Antiproliferative Activity, and Molecular Docking Studies
    (Taylor & Francis Ltd, 2022) Ersan, Ronak Haj; Alagoz, Mehmet Abdullah; Dogen, Aylin; Duran, Nizami; Burmaoglu, Serdar; Algul, Oztekin
    Four series of bisbenzoxazole derivatives were designed, synthesized, and screened for antiproliferative and antimicrobial activities. Generally, all synthesized bisbenzoxazoles (9-24) displayed significant antiproliferative activity; these effects were shown to be related to oxazole rings and substituents in bisbenzoxazole compounds. Especially, the series bearing chloro-substituent (9-12) exhibited better antiproliferative activity with higher selectivity than the other series (13-24); the IC50 values were observed in the range of 0.045-0.342 mu M. Interestingly, only the compound with a nitro substituent (22) showed maximum potency with an IC50 value of 0.011 mu M, which is two-fold more active than the standard drug methotrexate, with moderate selectivity. The compounds bearing fluoro-substituent (14-16) were found to exhibit potent antibacterial activity against the Gram-positive Enterococcus faecalis, with a MIC value of 62.5 mu g/mL, and moderate activity against Gram-negative bacteria and fungi. Only the compound 23 showed potent activity against Escherichia coli, with a MIC value of 62.5 mu g/mL. In order to better evaluate the activity results, crystal structures of five different proteins Human Anaplastic Lymphoma Kinase (PDB ID: 2XP2), CYP2C8dH complexed (PDB ID: 2NNI), factor-human kinase-beta enzyme IKK-beta enzyme (PDB ID: 4KIK), a tubulin heterodimer complex containing alpha and beta sub-units (PDB ID: 1Z2B) and penicillin-binding protein 4 (PBP4) from Enterococcus faecalis (PDB ID: 6MKI) were used in the docking study to examine antiproliferative and antimicrobial activity. Finally, an ADMET screening test was applied to determine the drug-like, toxicological, and optimum physicochemical properties for all of the synthesized compounds. The strategy applied in this research may act as a perspective for the rational design of potential anticancer drugs.
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    Design, synthesis and antiproliferative activity evaluation of fluorine-containing chalcone derivatives
    (Taylor & Francis Inc, 2022) Burmaoglu, Serdar; Aktas Anil, Derya; Gobek, Arzu; Kilic, Deryanur; Yetkin, Derya; Duran, Nizami; Algul, Oztekin
    A series of new chalcones containing fluoro atom at B ring have been designed, synthesized, and evaluated to be antiproliferative activity against a panel of human tumor cell lines. Some of the analogs (8, 9, 12, 45, 46 and 48) displayed powerful antiproliferative effects to certain human tumor cells, but all of them were devoid of any cytotoxicity towards the normal HEK 293. Acridine orange staining data supported that the cytotoxic and antiproliferative effects of the synthesized analogs on tumor cells are mediated through apoptosis. The compounds 12 and 46 manifested concentration-dependent antiproliferative activity in human hepatocellular carcinoma cell lines using an xCELLigence assay. The structures and antiproliferative activity relationship were further supported by in silico molecular docking study of the compounds against tubulin protein which suggests our compounds interference to cell division. Communicated by Ramaswamy H. Sarma
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    An efficient synthesis of novel di-heterocyclic benzazole derivatives and evaluation of their antiproliferative activities
    (Taylor & Francis Inc, 2021) Algul, Oztekin; Ersan, Ronak Haj; Alagoz, Mehmet Abdullah; Duran, Nizami; Burmaoglu, Serdar
    A series of unsymmetrical nine di-heterocyclic compounds of benzazole derivatives were synthesized at one step via cyclization reaction. The compounds evaluated forin vitrocytotoxic activity against A549, A498, HeLa, and HepG2 cancer cell lines. The biological evaluation results show that23, 26and29exhibit better activity against HepG2 and HeLa cancer cell lines. Compound23also showed good activity against A549, and A498 cancer cell lines. The analogs were further performed molecular docking studies against human cytochrome P450 2C8 monooxygenase enzyme, calculated some theoretical quantum parameters, ADMET descriptor and molecular electrostatic potential analysis. The strategy applied in this research work may act as a perspective for the rational design of potential anticancer drugs. Communicated by Ramaswamy H. Sarma
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    Head-to-head bisbenzazole derivatives as antiproliferative agents: design, synthesis, in vitro activity, and SAR analysis
    (Springer, 2021) Ersan, Ronak Haj; Alagoz, Mehmet Abdullah; Ertan-Bolelli, Tugba; Duran, Nizami; Burmaoglu, Serdar; Algul, Oztekin
    In the present work, a series of bisbenzazole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of these compounds was investigated using MTT assay. Bisbenzazole derivatives showed significant antiproliferative activity against all the four tested cancer cell lines. Among the various bisbenzazole derivatives, bisbenzoxazole derivatives exhibited the most promising anticancer activity followed by bisbenzimidazole and bisbenzothiazole derivatives. All the derivatives were found to be less toxic as compared to methotrexate (positive control) in normal human cells, indicating selective and efficient antiproliferative activity of these bisbenzazole derivatives. The structure-activity relationships of heteroaromatic systems and linkers present in bisbenzazole derivatives were analyzed in detail. In silico ADMET prediction revealed that bisbenzazole is a drug-like small molecule with a favorable safety profile. Compound31is a potential antiproliferative hit compound that exhibits unique cytotoxic activity distinct from methotrexate. [GRAPHICS]
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    Investigation of New Benzimidazole Derivative Compounds' Effects on A549 Cell Line
    (Inst Tecnologia Parana, 2020) Duran, Gulay Gulbol; Kucuk, Meral Urhan; Algul, Oztekin; Terzi, Menderes Yusuf
    Chronic inflammation is a common indication of several diseases, e.g. asthma, chronic obstructive pulmonary disease (COPD), atherosclerosis, etc. Benzimidazole derivatives are preferable compounds to design new analgesic and anti-inflammatory substances due to their unique biological features. We aimed to investigate the effect of a newly synthesized benzimidazole derivative, ORT-83, on A549 human lung adenocarcinoma cell line. ORT-83 was synthesized, and a non-cytotoxic concentration of ORT-83 on A549 cells was detected with MTT assay. To analyze the anti-inflammatory effect of ORT-83, an inflammatory cell culture model was established by stimulating A549 cell line with IL1-beta (10 ng/ml). After 2 hours of treatment with IL1-beta to induce inflammation, A549 cells were exposed to ORT-83 (0.78 mu g/ml) for 24 hours. Thereafter gene expression analyses were performed with qRT-PCR. We found that ORT-83 significantly suppressed the gene expression levels of the proinflammatory cytokines; IL-6, NFkB, and TNF-alpha. However, the increased levels of IL-10 (2.8 folds) by IL-1 beta induction did not change after ORT-83 and/or dexamethasone (Dex: positive control) treatments. While Dex; a COX-2 inhibitor, reduced the COX-2 expression level in inflammatory cells from 10.03 folds to 0.71 folds, ORT-83 reduced its level to 4.37 folds. iNOS expression levels did not change in any experimental groups. In conclusion, we showed that ORT-83 exerted its anti-inflammatory effects by repressing the gene expression of proinflammatory cytokines in the inflammation-induced A549 cell line. Although ORT-83 had a weaker COX-2 inhibitory effect compared to Dex, it was shown to be still a strong anti-inflammatory compound.
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    Synthesis and anti-proliferative activity of fluoro-substituted chalcones
    (Pergamon-Elsevier Science Ltd, 2016) Burmaoglu, Serdar; Algul, Oztekin; Anil, Derya Aktas; Gobek, Arzu; Duran, Gulay Gulbol; Ersan, Ronak Haj; Duran, Nizami
    A series of novel fluoro-substituted chalcone derivatives have been synthesized. All synthesized compounds were characterized by H-1 nuclear magnetic resonance (NMR), C-13 NMR, and elemental analysis. Their anti-proliferative activities were evaluated against five cancer cells lines, namely, A549, A498, HeLa, A375, and HepG2 using the MTT method. Most of the compounds showed moderate to high activity with IC50 values in the range of 0.029-0.729 mu M. Of all the synthesized compounds, 10 and 19 exhibited the most potent anti-proliferative activities against cancer cells, and 10 was identified as the most promising compound. (C) 2016 Elsevier Ltd. All rights reserved.
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    Synthesis and evaluation of antimicrobial activity of some 1,5(6)-H/or -methyl-2-subtituted benzimidazole derivatives
    (Chemical Publishing Co., 2007) Algul, Oztekin; Duran, Nizami; Gulbo, Gulay
    In this study, the investigation of structure-activitiy relationships for some newly synthesized benzimidazole structures was aimed. For this purpose, eight compounds having 1,5(6)-H/or -CH3 and 2-substituted benzimidazole structures were synthesized. Subsequently, their antimicrobial activities were examined. These compounds were tested in vitro against three Gram positive (Enterococcus faecalis, Staphylocccus aureus and Staphylocccus epidermidis) and two Gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa). In addition, they were screened in vitro for their antifungal activities. All of these compounds inhibited the growth of Gram positive and Gram negative bacteria at MIC values between 12.5 and 200 ?g/mL and had MIC values between 50 and 200 ?g/mL for the following fungi (Candida albicans, Candida krusei, Candida glabrata, Candida tropicalis and Candida parapsilosis).