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Öğe Antimicrobial activity evaluation of new 1,3,4-oxadiazole derivatives(University of Istanbul, 2017) Yurttaş, Leyla; Bülbül, Emre Fatih; Tekinkoca, Sinem; Demirayak, ŞerefIn this study, we have synthesized seven novel 2-[(5-(4-chlorobenzyl)-1,3,4-oxadiazol-2-yl)thio]-N-(6-substituted benzothiazol-2-yl)acetamide derivatives (4ag) starting from ethyl 4-chlorophenyl acetate. The antimicrobial acitivity of the compounds was screened against seven Gram positive and Gram negative bacteria and four fungi species; Escherichia coli ATCC 25922, Escherichia coli ATCC 35218, Enterococcus faecalis ATCC 51299, Enterococcus faecalis ATCC 29212, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Candida albicans, Candida krusei, Candida glabrata, Candida parapsilosis. Minumum inhibitor concentration (MIC) was calculated and compared with standard drugs, chloramphenicol and ketoconazole. Regarding the results of MIC, all compounds exhibited potency either at the higher concentrations or at the same concentrations compared with positive controls.Öğe Antimicrobial evaluation of trisubstituted 2-piperazinyl thiazoles(İstanbul Medipol University, 2019) Giray, Betül; Yurttaş, Leyla; Şahin, Zafer; Berk, Barkın; Demirayak, ŞerefThiazole and basic nitrogen containing rings are important chemical moieties of antimicrobial drugs. In recent, third generation cephalosporins include thiazole ring system. In this study, we synthesized 33 piperazine thiazole derivatives which were thought to show antimicrobial activity. Synthesize were realized with good yield using the method which reports the anticholinesterase properties of these compounds. Similar compounds with the same scaffold (2, 4, 5 trisubstituted thiazoles) are investigated for antimicrobial activity. Compounds 23-27 exhibited MIC: 256 µM against S. aureus ATCC 25923. Besides, 27-33 group showed MIC: 256 µM against K. pneumoniae UC57 and B. cereus. It is remarkable that the compound 27 showed antimicrobial activity against 4 different microorganisms and 26 showed antimicrobial activity against L. monocytogenes by MIC: 32 µM which is same as the standart chloramphenicol.Öğe Cytotoxic, antiproliferative and apoptotic effects of new benzimidazole derivatives on A549 lung carcinoma and C6 glioma cell lines(Bentham Science Publishers, 2015) Yurttaş, Leyla; Demirayak, Şeref; Çiftçi, Gülşen AkalınBenzimidazole ring is a versatile structure which has been extensively utilized in medicinal chemistry. Since we are working on 1,2-disubstutited benzimidazoles, we have reported new antitumor active derivatives. As a continuation to our previous work, we have synthesized a new series of 1-(2-aryl-2-oxoethyl)-2-[(N,N- dimethylamino/pyrrolidinyl/piperidinyl)thiocarbamoyl] benzimidazole derivatives. Anticancer activity of the compounds was evaluated using MTT assay, BrdU assay and flow cytometric analysis on A549 human lung carcinoma and C6 rat glioma cell lines. Compounds bearing dimethylamino moiety exhibited higher antitumor activity.Öğe Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors(Taylor & Francis Ltd, 2020) Şahin, Zafer; Biltekin, Sevde Nur; Bülbül, Emre Fatih; Yurttaş, Leyla; Berk, Barkın; Demirayak, ŞerefNewly synthesized 4-substituted phenyl-2-(4-substituted phenylpiperazine-1-yl)thiazole derivatives (4a-v) were evaluated in terms of their acetylcholinesterase (AChE) inhibition activities. Twenty-two compounds were tested against AChE at six different concentrations that varied between 10(-4)and 10(-9) M. The concentrations that inhibited AChE were calculated between 1.15 and 3.45 mu M in seven compounds (4a,4b,4h,4l,4m,4q,4r). Compounds4m,4b, and4lrepresented 1.15, 1.31, 1.34 mu M (IC50) inhibitions, respectively. Although the inhibition values are lower than that of donepezil, they are considerable. Modeling studies of these analogs revealed similar positioning with donepezil, in which Ar-Ar interactions with Tyr337 and Trp 286 exist.Öğe Discovery of novel potent human chondrosarcoma (SW1353) inhibitors: 4-(2/3/4-pyridyl)thiazole 2-acetamide derivatives(Elsevier B.V., 2023) Coşkun, Göknil Pelin; Şahin, Zafer; Erdoğan, Ömer; Çevik, Özge; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Ülgen, Mert; Demirayak, ŞerefChondrosarcoma is the most common cartilage sarcoma among adult patients. It is mainly observed after the degradation of chondrocytes in the case of cell stress. Unfortunately, the mortality among patients is high as a result of metastasis. Here in this study we have discovered some novel 4-(2/3/4-pyridyl)thiazole2-acetamide derivatives and elucidated their structure using chromatographic and spectroscopic methods. The antitumor activity profile for the synthesized compounds was performed using an MTT assay and apoptotic pathways (BAX, BCL-2) on the chondrosarcoma (SW1353) cell line. Besides, tyrosine kinase activity studies were also performed in order to understand the underlying mechanism of action. Among the synthesized compounds, there are some compounds showed excellent activity on chondrosarcoma cells. Besides, compounds showed no cytotoxicity on healthy fibroblast (L929) cell lines. Among the compounds, the compound having benzimidazole moiety showed the highest activity with IC50 value of 2.03±1.05 µM compared to doxorubicin (5.05±1.07 µM). The results indicated that the anticancer activity of the compounds might be depending on tyrosine kinase inhibiton. The compounds are also exhibited to induce apoptosis in chondrosarcoma cells. Morphological and colony observations are also successfully visualized.Öğe In vitro antitumor activity evaluation of some 1,2,4-triazine derivatives bearing piperazine amide moiety against breast cancer cells(Elsevier Ltd, 2014) Yurttaş, Leyla; Demirayak, Şeref; Ilgın, Sinem; Atlı, ÖzlemA series of 1,2,4-triazine derivatives bearing piperazine amide moiety has been synthesized and investigated for their potential anticancer activities. 1-[4-(5,6-Bis (4-subtituted phenyl) -1,2,4-triazin-3-yl)piperazin-1-yl]-2-[4-(3-substituted phenyl) piperazin-1-yl]ethanone derivative (1-32) compounds were synthesized by a four step synthetic procedure. The activity studies were evaluated using XTT method, BrdU method and flow cytometric analysis on MCF-7 breast cancer cells and NIH/3T3 (mouse embryonic fibroblast cells) healthy cells. Compounds 5 with 3-chlorophenyl and compound 7 with 4-chlorophenyl substitutions were found to be promising antiproliferative agents comparing with an effective anticancer drug, cisplatin.Öğe Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a] benzimidazole derivatives and investigation of their anticancer activities(Elsevier, 2011) Demirayak, Şeref; Kayagil, İsmail; Yurttaş, LeylaThe syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities.Öğe New chroman-4-one/thiochroman-4-one derivatives as potential anticancer agents(Elsevier Science Bv, 2017) Demirayak, Şeref; Yurttaş, Leyla; Gündoğdu-Karaburun, Nalan; Karaburun, Ahmet Çagrı; Kayagil, İsmailThe synthesis of 3-[3/4-(2-aryl-2-oxoethoxy) arylidene] chroman/thiochroman-4-one derivatives (1-34) and evaluation of their anticancer activities were aimed in this work. Final compounds were obtained in multistep synthesis reactions using phenol/thiophenol derivatives as starting materials. For anticancer activity evaluation, all compounds were offered to National Cancer Institute (NCI), USA and selected ones were tested against sixty human tumor cell lines derived from nine neoplastic diseases. The activity results were evaluated according to the drug screening protocol of the institute. Compounds containing thiochromanone skeleton exhibited higher anticancer activity.Öğe Novel benzimidazole derivatives: Cytotoxic and apoptotic properties on lung cancer cell line(Bentham Science Publishers, 2020) Yurttaş, Leyla; Akalın Çiftçi, Gülşen; Aksoy, Mehmet Onur; Demirayak, ŞerefBackground: Benzimidazole derivatives are privileged molecules known to have a wide variety of biological activities. In medicinal chemistry, due to the ring's structural similarity to nucleotides, its derivatives were investigated as new chemotherapeutic agents. Our research group have been studying 1,2-disubstituted benzimidazoles, including thiocarbamoyl group and their potential anticancer activity. Based on previous findings, we synthesized novel 1-[2-(4-substituted phenyl-2-oxoethyl)]-2-[(2/3/4-substituted phenylpiperidin-1-yl)thiocarbamoyl]benzimidazole derivatives (3a-o).Methods: The obtained fifteen derivatives were studied on A549 adenocarcinomic human alveolar basal epithelial cell line and mouse L929 fibroblastic cell line to determine their cytotoxic activity. These compounds were also investigated to identify their apoptotic properties.Results and Discussion: The structures of the compounds based on three different groups differ from each other with the phenyl substituents bonded to the piperazine ring. All of the compounds showed remarkable antitumor activity, but the first five compounds bearing non-substituted phenyl moiety exhibited selective cytotoxicity when compared in terms of potencies to the normal cell line.Conclusion: Compounds 3j, 3m and 3n were identified as the most apoptotic derivatives; however, compounds 3e and 3h provoked apoptosis with the percentages of 10.6 and 10.9% and selective cytotoxicity.Öğe Novel benzofurane carbonyl analogs of donepezil as acetylcholinesterase inhibitors(Elsevier B.V., 2022) Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Küçükkılınç, Tuba Tüylü; Demirayak, ŞerefDonepezil is the most prescribed drug for mild to moderate Alzheimer's Disease. There is not any alternative drug with this potency yet. New scaffolds bearing benzofurans and amines are being tested for good potency on acetylcholinesterase enzyme to mimic donepezil. In this study, we synthesized 22 novel compounds (2a-b, 3a-t) namely benzofuroyl-phenylpiperazines with 3 step reaction having one microwave green synthesis step at first. Compounds were tested with a modified Ellmann method on cholinesterases. Molecular modeling studies were performed on human acetylcholinesterase X-ray crystal structure complexed with donepezil (4EY7) using Maestro Schrödinger. The most active compounds were subjected to a ?-amyloid disaggregation assay. All tested compounds showed good activity (except 3n-p bearing Cl on benzofurane) on acetylcholinesterase (0.98–54 µM) and most of the compounds showed a one-digit IC50, where donepezil was 0.12 µM. The most active compounds according to IC50 values were 3t: 0.98 µM, 3s:1.07 µM, 2b:1.08 µM and 2a: 1.14 µM. Besides, compounds did not show significant activity on butyrylcholinesterase at 100 µM. Molecular modeling studies of compounds showed a good consistency (rmsd=0.45) with the binding mode and interactions of donepezil. 2b, 3 s and 3t exhibited good disaggregation potential on 1–40 ?-amyloid. Compound 3t disaggregated more than standard drug rifampicin. Cytotoxicity test results on HEK293 (at 50 µM), showed lower cytotoxicity (except for 3j-k) compared to cisplatin (46% viability). Promisingly, the most active compounds on AChE, 2a-b and 3q-t, showed the lowest cytotoxicity (64–74% viability). Consequently, we have developed potent inhibitors of AChE with close activity to donepezil. For enzyme activity; the presence of methoxy on the aromatic site, ionizable nitrogen group and a carbonyl group on/nearly to main ring (benzofurane) asserted essentially to develop more potent compounds that are equivalent to donepezil.Öğe Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation(Walter de Gruyter GmbH, 2022) Şahin, Zafer; Özhan, Yağmur; Sipahi, Hande; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Demirayak, ŞerefNovel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with alpha-hydroxy aldehyde or alpha-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by H-1 NMR, C-13 NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 mu M and 8.0 mu M IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 mu M IC50. Rest of the compounds (1, 3-9) showed 10.4-28.1 mu M IC50 on COX-2 and 17.0-35.6 mu M IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1-9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 mu M for all compounds (1-9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.Öğe Novel benzothiazole based imidazole derivatives as new cytotoxic agents against glioma (C6) and liver (HepG2) cancer cell lines(University of Istanbul, 2017) Yurttaş, Leyla; Ertaş, Merve; Akalın Çiftçi, Gülşen; Temel, Halide Edip; Demirayak, ŞerefIn this work, some novel N-(6-substituted-benzothiazol-2-yl)-2-[[4,5-dimethyl-1-((p-tolyl/4-nitrophenyl)amino)-1H-imidazol-2-yl]thio]acetamide derivatives were synthesized and searched for their cytotoxic activities against C6 and HepG2 tumor cells. Among all compounds, the most active compound was determined as compound 7. It was calculated IC50 value about 15.67 µg/mL through C6 tumor cell lines and also compound 2, 4, 5, 6 were observed as good cytotoxic agents against HepG2 tumor cells. Findings about antiproliferative activity studies have encouraged the acquirement of new similar compounds in undergoing studies.Öğe Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition(Elsevier France-Editions Scientifiques Medicales Elsevier, 2021) Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Özhan, Yağmur; Sipahi, Hande; Gao, Zhanguo; Jacobson, Kenneth A.; Demirayak, ŞerefThiouracil and thiocytosine are important heterocyclic pharmacophores having pharmacological diversity. Antitumor and antiviral activity is commonly associated with thiouracil and thiocytosine derivatives, which are well known fragments for adenosine receptor affinity with many associated pharmacological properties. In this respect, 33 novel compounds have been synthesized in two groups: 24 thiouracil derivatives (4a-x) and 9 thiocytosine derivatives (5a-i). Antitumor activity of all the compounds was determined in the U87 MG glioblastoma cell line. Compound 5e showed an anti-proliferative IC50 of 1.56 ?M, which is slightly higher activity than cisplatin (1.67 ?M). The 11 most active compounds showed no signficant binding to adenosine A1, A2A or A2B receptors at 1 ?M. Brain tumors express high amounts of phosphodiesterases. Compounds were tested for PDE4 inhibition, and 5e and 5f showed the best potency (5e: 3.42 ?M; 5f: 0.97 ?M). Remakably, those compounds were also the most active against U87MG. However, the compounds lacked a cytotoxic effect on the HEK293 healthy cell line, which encourages further investigation.Öğe Novel thiazole-piperazine derivatives as potential cholinesterase inhibitors(Wiley, 2019) Demirayak, Şeref; Şahin, Zafer; Ertaş, Merve; Bülbül, Emre Fatih; Bender, Ceysu; Biltekin, Sevde Nur; Berk, Barkın; Sağlık, Begüm Nurpelin; Levent, Serkan; Yurttaş, LeylaDementia is a cognitive disorder mostly associated with Alzheimer's disease (AD) in addition to being seen in many other diseases of the central nervous system (CNS). The limited number of drugs is not sufficient to provide adequate improvement to increase the quality of life of patients suffering from this symptom; therefore, all treatment options should be evaluated in detail. In this study, new molecules, [2-(4-(2/3/4-substituted phenyl)piperazin-1-yl)-4-phenylthiazol-5-yl][3/4-substituted phenyl]methanone derivatives (1-44), were obtained and analyzed in terms of their anticholinesterase activities. Kinetic mode and molecular interactions were also evaluated. An enzyme inhibition study was undertaken on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the Ellman method. Maestro program was used in molecular modeling studies. Forty-four compounds were evaluated on AChE and BChE enzymes at 10(-3) and 10(-4) concentrations. The inhibition concentrations were calculated as 0.268 mu M to 2.104 mu M for six compounds (4, 5, 16, 27, 37, and 38) on AChE. Compound 5 including the 4-methoxy substituent (IC50: 0.268 mu M) and compound 38 containing the 4-methoxy and 3-methyl substituents (IC50: 0.286 mu M) showed the highest AChE inhibitory activity. They were further examined in terms of hydrogen bonding with Arg296 and Ar-Ar interaction with Trp286. The activity of compound 5 was also assessed in mixed-type kinetic mode.Öğe Potent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives(Wiley, 2019) Ertaş, Merve; Şahin, Zafer; Bülbül, Emre Fatih; Bender, Ceysu; Biltekin, Sevde Nur; Berk, Barkın; Yurttaş, Leyla; Nalbur, Aysu M.; Çelik, Hayati; Demirayak, ŞerefThe antioxidant, antimalarial, antibacterial, and antitumor activities of thiosemicarbazones have made this class of compounds important for medicinal chemists. In addition, thiosemicarbazones are among the most potent and well-known ribonucleotide reductase inhibitors. In this study, 24 new thiosemicarbazone derivatives were synthesized, and the structures and purity of the compounds were determined by IR, H-1 NMR, C-13 NMR, mass spectroscopy, and elemental analysis. The IC50 values of these 24 compounds were determined with an assay for ribonucleotide reductase inhibition. Compounds 19, 20, and 24 inhibited ribonucleotide reductase enzyme activity at a higher level than metisazone as standard. The cytotoxic effects of these compounds were measured on the MCF7 (human breast adenocarcinoma) and HEK293 (human embryonic kidney) cell lines. Similarly, compounds 19, 20, and 24 had a selective effect on the MCF7 and HEK293 cell lines, killing more cancer cells than cisplatin as standard. The compounds (especially 19, 20, and 24 as the most active ones) were then subjected to docking experiments to identify the probable interactions between the ligands and the enzyme active site. The complex formation was shown qualitatively. The ADME (absorption, distribution, metabolism, and excretion) properties of the compounds were analyzed using in-silico techniques.Öğe Pyridine-substituted thiazolylphenol derivatives: Synthesis, modeling studies, aromatase inhibition, and antiproliferative activity evaluation(Wiley-VCH Verlag, 2018) Ertaş, Merve; Şahin, Zafer; Berk, Barkın; Yurttaş, Leyla; Biltekin, Sevde Nur; Demirayak, ŞerefDrugs used in breast cancer treatments target the suppression of estrogen biosynthesis. During this suppression, the main goal is to inhibit the aromatase enzyme that is responsible for the cyclization and structuring of estrogens either with steroid or non-steroidal-type inhibitors. Non-steroidal derivatives generally have a planar aromatic structure attached to the triazole ring system in their structures, which inhibits hydroxylation reactions during aromatization by coordinating the heme group. Bioisosteric replacement of the triazole ring system and development of aromatic/cyclic structures of the side chain can increase the selectivity for aromatase enzyme inhibition. In this study, pyridine-substituted thiazolylphenol derivatives, which are non-steroidal triazole bioisosteres, were synthesized using the Hantzsch method, and physical analysis and structural determination studies were performed. The IC50 values of the compounds were determined by a fluorescence-based aromatase inhibition assay. Then, their antiproliferative activities on the MCF7 and HEK 293 cell lines were evaluated with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Furthermore, the crystal structure of human placental aromatase was subjected to a series of docking experiments to identify the possible interactions between the most active structure and the active site. Lastly, an in silico technique was performed to analyze and predict the drug-likeness, molecular and ADME properties of the synthesized molecules.Öğe Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives(Pergamon-Elsevier Science Ltd, 2018) Şahin, Zafer; Ertaş, Merve; Berk, Barkın; Biltekin, Sevde Nur; Yurttaş, Leyla; Demirayak, ŞerefSteroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on developing non-steroidal derivatives for their potential clinical use avoiding steroidal side-effects. Non-steroidal derivatives generally have planar aromatic structures attached to the azole ring system. One part of this ring system comprises functional groups that inhibit aromatization through the coordination of the haem group of the aromatase enzyme. Replacement of the triazole ring system and development of aromatic/cyclic structures of the side chain can increase selectivity over aromatase enzyme inhibition. In this study, 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl) thiazole derivatives were synthesized and physical analyses and structural determination studies were performed. The IC50 values were determined by a fluorescence-based aromatase inhibition assay and compound 1 (4-(2-hydroxyphenyl)-2-(pyrimidine-2-yl) thiazole) were found potent inhibitor of enzyme (IC50: 0.42 nM). Then, their antiproliferative activity over MCF-7 and HEK-293 cell lines was evaluated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Compounds 1, 7, 8, 13, 15, 18, 21 were active against MCF-7 breast cancer cells. Lastly, a series of docking experiments were undertaken to analyze the crystal structure of human placental aromatase and identify the possible interactions between the most active structure and the active site.Öğe Synthesis and anti-cancer activity evaluation of new aurone derivatives(Taylor and Francis, 2015) Demirayak, Şeref; Yurttaş, Leyla; Gündoğdu Karaburun, Nalan; Karaburun, Ahmet Çağrı; Kayagil, İsmailIn this study, we have synthesized 2-[3-or 4-(2-aryl-2-oxoethoxy) arylidene] benzofuran-3-one derivatives (D1-D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1-A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1-C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with a-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.Öğe Synthesis and antibacterial evaluation of novel benzimidazole, benzothiazole, benzofurane, and naphtofurane derivatives of aminothiazoles(Ankara Association of Pharmaceutical Sciences, 2022) Şahin, Zafer; Tok, Büşra Işıl; Akgün, Erol; Çaşkurlu, Ayşegül; Yurttaş, Leyla; Berk, Barkın; Demirayak, ŞerefThe thiazole ring is the core of bioactive molecules that generate broad activity. These activities include anticonvulsant, antimicrobial, antituberculosis, antiviral, etc. In this work, starting from seconder/cyclic amines, new compounds containing thiazole and benzimidazole/benzothiazole/benzofurane/naphtofurane rings were synthesized, and their antimicrobial effects were evaluated. 9 compounds were synthesized by converting the seconder and cyclic amines to thiourea, and continued by thiazole ring closure. Ring closure was achieved by methylene-carbonyl condensation except conventional methods. Compound characterization was realized by FT-IR, 1 H NMR and 13C NMR and HRMS. Compounds did not show significant activity on bacterial strains. Nine aminothiazole derivatives have been synthesized successfully. Compounds did not show important antibacterial activity and thus were evaluated as inactive.Öğe Synthesis and anticancer activity of some 1H-inden-1-one substituted (heteroaryl)acetamide derivatives(Bentham Science Publishers Ltd., 2019) Karaburun, Ahmet Çağrı; Gündoğdu-Karaburun, Nalan; Yurttaş, Leyla; Kayagil, İsmail; Demirayak, ŞerefBackground: The synthesis of 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2ylidene) methyl)phenoxy]-N-(heteroaryl)acetamide derivatives and the investigation of their anticancer activity were studied. Methods: 2-(3/4-Hydroxybenzylidene)-6-substituted-2,3-dihydro-1H-inden-1-ones were reacted with suitable 2-chloroacetamides to give 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2-ylidene)methyl) phenoxy]-N-(heteroaryl) acetamide derivatives. Results: The structure elucidation of the newly synthesised 16 compounds was performed by IR, 1H-NMR, mass spectroscopic data and elemental analyses. The anticancer screening was carried out in National Cancer Institute (NCI), USA. Conclusion: Compound 3e (2-(3-((6-chloro-1-oxo-2,3-dihydro-1H-inden-2-ylidene) methyl)phenoxy)N-(thiazol-2-yl)acetamide), exhibited highest growth inhibition against the leukaemia (61.47%), non-small cell lung cancer (79.31%) and breast cancer (62.82%) cell lines.
