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Full-Text Articles in Physical Sciences and Mathematics
Structure-Activity Relationship Of Anticancer Drug Candidate Quinones, Nadire Özenver, Neslihan Sönmez, Merve Yüzbaşıoğlu Baran, Ayşe Uz, Lütfiye Ömür Demi̇rezer
Structure-Activity Relationship Of Anticancer Drug Candidate Quinones, Nadire Özenver, Neslihan Sönmez, Merve Yüzbaşıoğlu Baran, Ayşe Uz, Lütfiye Ömür Demi̇rezer
Turkish Journal of Chemistry
Breast cancer is one of the most prevalent cancer types worldwide. Chemotherapy is a substantial approach in the management of breast cancer despite the occurrence of chemotherapy-associated side effects and the development of multidrug resistance in cancer cells. At this point, a variety of quinone derivatives may represent potential as possible anticancer drug candidates due to possessing structural similarity towards clinically used anticancer drugs like doxorubicin. Therefore, we investigated the cytotoxic effects of various quinone derivatives with structural diversity towards a variety of breast cancer cells. We further determined their toxicity in healthy cells to evaluate their drug capability potential. …
Synthesis Of New Imine-/Amine-Bearing Imidazo[1,2-A]Pyrimidine Derivatives And Screening Of Their Cytotoxic Activity, Tuğba Güngör, Hazal Nazlican Atalay, Yakup Berkay Yilmaz, Tuğba Tümer, Mehmet Ay
Synthesis Of New Imine-/Amine-Bearing Imidazo[1,2-A]Pyrimidine Derivatives And Screening Of Their Cytotoxic Activity, Tuğba Güngör, Hazal Nazlican Atalay, Yakup Berkay Yilmaz, Tuğba Tümer, Mehmet Ay
Turkish Journal of Chemistry
Imidazo[1,2-a]pyrimidine derivatives bearing imine groups (3a-e) were successfully synthesized in moderate to good yields using microwave-assisted heating. Corresponding amine derivatives (4a-e) were also obtained by the reduction reaction of the imine derivatives (3a-e). All synthesized products were characterized by FT-IR, 1 H NMR, 13C NMR, and LC-MS spectroscopic techniques. In silico ADMET, Lipinski, and drug-likeness studies of the compounds were conducted and all were found to be suitable drug candidates. The cytotoxicity of the potential drug molecules was screened against the breast cancer cell lines MCF-7 and MDA-MB-231 and the healthy model HUVEC by the sulforhodamine B method. According to …
Comprehensive Evaluation Of Reseda Lutea L. (Wild Mignonette) And 7 Isolated Flavonol Glycosides: Determination Of Antioxidant Activity, Anti-Alzheimer, Antidiabetic And Cytotoxic Effects With In Vitro And In Silico Methods, Hati̇ce Kiziltaş
Turkish Journal of Chemistry
In this study, anticholinergic, antidiabetic, antioxidant and cytotoxic activities of Reseda lutea L. (R. lutea) were determined. Ethanol extracts of R. lutea (EERL) and water extract of R. lutea (WERL) were prepared for biochemical analysis. The antioxidant capacities of EERL and WERL were evaluated with 6 different methods. In addition, acetylcholinesterase (AChE), α-amylase and α-glycosidase enzyme inhibition by EERL were measured. According to the results, EERL exhibited high inhibition effects against α-amylase, α-glycosidase and AChE enzymes. The IC50 values of EERL against AChE (2.21 μg/mL), α-glycosidase (1.38 μg/mL), and α-amylase (0.11 μg/mL) were determined. Also, high cytotoxic effect of EERL …
Major Chemical Constituents From Illicium Griffithii Hook. F. & Thoms Of North East India And Their Cytotoxicity And Antimicrobial Activities, Deepjyoti Dutta, Bardwi Narzary, Snigdha Saikia, Kashyap J. Tamuli, Manobjyoti Bordoloi, Neipihoi Lhouvum, Shyamalendu Nath, Ranjan K. Sahoo, Barnali Gogoi, Surovi Saikia, Nayan K. Bhattacharyya
Major Chemical Constituents From Illicium Griffithii Hook. F. & Thoms Of North East India And Their Cytotoxicity And Antimicrobial Activities, Deepjyoti Dutta, Bardwi Narzary, Snigdha Saikia, Kashyap J. Tamuli, Manobjyoti Bordoloi, Neipihoi Lhouvum, Shyamalendu Nath, Ranjan K. Sahoo, Barnali Gogoi, Surovi Saikia, Nayan K. Bhattacharyya
Turkish Journal of Chemistry
Illicium griffithii Hook. f. & Thoms is an endemic medicinal plant of North East India found in the Eastern Himalayan region of biodiversity mega centre. Herein, chemical investigation of I. griffithii, afforded five compounds and their structures were determined through extensive use of NMR, HRMS, and FT-IR spectroscopy. The complete proton-proton, proton-carbon coupling network of compound 1 was determined using 1H-1H COSY, HSQC and NOESY NMR experiments. All the compounds were evaluated for their cytotoxic activity by MTT assay and antimicrobial activity by Agar well diffusion method. Compound 1 exhibited significant cytotoxicity activity against Lung cancer (A549) and pancreatic …
Thio-Schiff Bases Derived From 2,2'-Disulfanedianiline Via Nanocerium Oxide: Antimicrobial Effect And Antiproliferative Effects In Melanoma Cells, Aslihan Dalmaz, Sefa Durmuş, Görkem Dülger, Merve Alpay
Thio-Schiff Bases Derived From 2,2'-Disulfanedianiline Via Nanocerium Oxide: Antimicrobial Effect And Antiproliferative Effects In Melanoma Cells, Aslihan Dalmaz, Sefa Durmuş, Görkem Dülger, Merve Alpay
Turkish Journal of Chemistry
In this study, the synthesis of dimeric disulfide-Schiff bases was carried out using two methods. The structures of the obtained Schiff bases were elucidated by various spectroscopic methods as well as elemental analysis. The Schiff base derivative compounds (3a-6) were screened for in vitro antibacterial activity against multidrug-resistant microorganisms using microdilution method. All the tested compounds showed varying inhibition zones against the pathogens. According to MIC results, the compound 2 was shown strong inhibitory activity against all the tested microorganisms compared to antibiotics. In addition, all the tested compounds showed different antiproliferative effects on the melanoma cell line (B16F10). Our …
Investigation Of Boron Nanosized Particles Prepared With Various Surfactants And Chitosan In Terms Of Physical Stability And Cell Viability, Emrah Özakar, Mehmet Semi̇h Bi̇ngöl, Ruki̇ye Sevi̇nç Özakar
Investigation Of Boron Nanosized Particles Prepared With Various Surfactants And Chitosan In Terms Of Physical Stability And Cell Viability, Emrah Özakar, Mehmet Semi̇h Bi̇ngöl, Ruki̇ye Sevi̇nç Özakar
Turkish Journal of Chemistry
Nanosuspensions (NS) are one of the new generation drug carrier forms developed to overcome the deficiencies of drugs with poor water solubility or insolubility and are considered to be one of the most successful approaches to formulate compounds in recent years. Boron nitride (BN) is insoluble in water and chemically more stable than carbon, it offers better biological superiority although the application of carbon structures in the biomedical field has increased in recent years. Chitosan is a polymer with excellent processability and biocompatibility thanks to its high dielectric constant. In addition, chitosan has a high affinity for metal ions. This …
Release Of Nifedipine, Furosemide, And Niclosamide Drugs From The Biocompatible Poly(Hema) Hydrogel Structures, Bahar Yilmaz
Release Of Nifedipine, Furosemide, And Niclosamide Drugs From The Biocompatible Poly(Hema) Hydrogel Structures, Bahar Yilmaz
Turkish Journal of Chemistry
The primary aim of this article was to improve the solubility and bioavailability of the drugs nifedipine, niclosamide, and furosemide due to their poor solubility and dissolution rate. Therefore, these drugs require improvement in solubility and dissolution rate in formulation development, especially in solid dosage forms such as hydrogels and capsules. Hydrogel structures were synthesized by using a biocompatible, nontoxic, and protective pure 2-hydroxy ethyl methacrylate (HEMA) monomer. These hydrogel structures were characterized by various techniques such as scanning electron microscopy and Fourier-transformed infrared spectroscopy. In the next step, drug molecules were loaded in the poly (HEMA) hydrogels. Drug releases …
Synthesis And Characterization Of Magnetic Nanocomposite For In Vitro Evaluation Of Irinotecan Using Human Cell Lines, Tuba Tarhan
Synthesis And Characterization Of Magnetic Nanocomposite For In Vitro Evaluation Of Irinotecan Using Human Cell Lines, Tuba Tarhan
Turkish Journal of Chemistry
In this study, magnetic O-carboxymethyl chitosan (MOCC) nanocomposite was synthesized and characterized as a drug delivery system for loading the anticancer drug irinotecan (CPT-11). To increase the drug loading capacity, MOCC was synthesized by linking the carboxyl group functionally to chitosan. Also, several critical factors such as concentration, the dose of MOCC, and contact time for optimum drug loading condition were investigated. The loading capacity of CPT-11 onto MOCC was calculated as 5.6 mg/g, and the loaded drug concentration was calculated as 0.04787 mM at pH value of 5. Besides, the cytotoxic properties of MOCC, CPT- 11 loaded MOCC (MOCC-CPT-11), …
Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç
Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç
Turkish Journal of Chemistry
The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure with 1H NMR, 13C NMR and FT-IR spectral foundations, which were compatible with literature informations. Antimicrobial activity and cytotoxicity studies were done by disc diffusion and NCI-60 sulphordamine B assay methods. The antimicrobial test results revealed that synthesized compounds have better activity against gram-positive species than gram-negative ones. A total analysis of the antibacterial, antifungal, and antiyeast activity revealed that newly synthesized compounds were really active against Bacillus cereus, Bacillus …
Investigation Of Olea Ferruginea Roylebark Extracts For Potential In Vitroantidiabetic And Anticancer Effects, Samra Liaqat, Muhammad Islam, Hamid Saeed, Mehwish Iqtedar, Azra Mehmood
Investigation Of Olea Ferruginea Roylebark Extracts For Potential In Vitroantidiabetic And Anticancer Effects, Samra Liaqat, Muhammad Islam, Hamid Saeed, Mehwish Iqtedar, Azra Mehmood
Turkish Journal of Chemistry
This study was conducted to investigate the physicochemical, phytochemical, in vitro antidiabetic and anticancer potential of Olea ferruginea R bark. After extraction using Soxhlet, in vitro antidiabetic and cytotoxic activity on human hepatocellular carcinoma (HepG2) cells was assessed by nonenzymatic glycosylation of hemoglobin assay, alpha-amylase inhibition assay, glucose uptake by yeast cells, and 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay, respectively, and gene expression via real-time polymerase chain reaction. Primary and secondary metabolites were present in the extractants; polyphenols (35.61 ± 0.03) and flavonoids (64.33 ± 0.35) in the chloroform; and polysaccharides in the ethanol (268.75 ± 0.34), and glycosaponins (78.01 ± …
Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n
Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n
Turkish Journal of Chemistry
Cancer is a disease characterized by the continuous growth of cells without adherence to the rules that healthy normal cells obey. Carbonic anhydrase I and II (CA I and CA II) inhibitors are used for the treatment of some diseases. The available drugs in the market have limitations or side effects, which bring about the need to develop new drug candidate compound(s) to overcome the problems at issue. In this study, new pyrazole-sulphonamide hybrid compounds 4-[5-(1,3-benzodioxol-5-yl)-3-aryl-4,5-dihydro-1Hpyrazol- 1-yl]benzenesulphonamides (4a - 4j) were designed to discover new drug candidate compounds. The compounds 4a - 4j were synthesized and their chemical structures were …
Synthesis, Cytotoxic Assessment, And Molecular Docking Studies Of2,6-Diaryl-Substituted Pyridine And 3,4- Dihydropyrimidine-2(1h)-One Scaffolds, Zahra Hosseinzadeh, Nima Razzaghi-Asl, Ali Ramazani, Hamideh Aghahosseini, Ali Ramazani
Synthesis, Cytotoxic Assessment, And Molecular Docking Studies Of2,6-Diaryl-Substituted Pyridine And 3,4- Dihydropyrimidine-2(1h)-One Scaffolds, Zahra Hosseinzadeh, Nima Razzaghi-Asl, Ali Ramazani, Hamideh Aghahosseini, Ali Ramazani
Turkish Journal of Chemistry
Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytotoxic effects against several cancer cell lines. An easy and convenient method is reported for the synthesis of these derivatives, employing cobalt ferrite (CoFe$_{2}$ O$_{4}$ @SiO$_{2}$ -SO$_{3}$ H) magnetic nanoparticles under microwave irradiation and solvent-free conditions. The structural characteristics of the prepared nanocatalyst were investigated by FTIR, XRD, SEM, and TGA techniques. In vitro cytotoxic effects of the synthesized products were assessed against the human breast adenocarcinoma cell line …
Design, Synthesis, Cytotoxic Activity, And Apoptosis Inducing Effects Of 4- And N-Substituted Benzoyltaurinamide Derivatives, Özlem Akgül, Mümi̇n Alper Erdoğan, Dervi̇ş Bi̇ri̇m, Çağla Kayabaşi, Cumhur Gündüz, Güli̇z Armagan
Design, Synthesis, Cytotoxic Activity, And Apoptosis Inducing Effects Of 4- And N-Substituted Benzoyltaurinamide Derivatives, Özlem Akgül, Mümi̇n Alper Erdoğan, Dervi̇ş Bi̇ri̇m, Çağla Kayabaşi, Cumhur Gündüz, Güli̇z Armagan
Turkish Journal of Chemistry
In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test. Compound 14 (in SH-SY5Y and MDA-MB-231 cell lines) and 15 (in SH-SY5Y cell line) were found to induce intrinsic …
Anticancer And Antiangiogenesis Activities Of Novel Synthesized 2-Substituted Benzimidazoles Molecules, Adem Güner, Eli̇fsu Polatli, Tamer Akkan, Hakan Bektaş, Canan Albay
Anticancer And Antiangiogenesis Activities Of Novel Synthesized 2-Substituted Benzimidazoles Molecules, Adem Güner, Eli̇fsu Polatli, Tamer Akkan, Hakan Bektaş, Canan Albay
Turkish Journal of Chemistry
In this study, novel 2-substituted benzimidazoles molecules having triazole, thiadiazole, and oxadiazole rings were synthesized and were evaluated by anticancer, antioxidant/oxidant status, genotoxicity, and antiangiogenesis assays. Anticancer activity of the compounds was determined by MTT (0.5, 5, and 50 $\mu $g/mL) and lactate dehydrogenase (LDH) release assays against human prostate and breast cancer cells. Oxidative status of cells was elicited by total oxidative stress and total antioxidant capacity methods. Chick chorioallantoic membrane assay was used to evaluate the antiangiogenic activity. Genotoxicity was evaluated by the sister chromatid exchange (SCE) and micronucleus (MN) tests in lymphocyte cultured human blood. Our results …
Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel
Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel
Turkish Journal of Chemistry
A 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 …
Synthesis And Cytotoxicity Evaluation Of [(2,4-Dichlorophenoxy)Methyl]-5-Aryl-1,3,4-Oxadiazole/4$H$-1,2,4-Triazole Analogues, Mohamed Jawed Ahsan
Synthesis And Cytotoxicity Evaluation Of [(2,4-Dichlorophenoxy)Methyl]-5-Aryl-1,3,4-Oxadiazole/4$H$-1,2,4-Triazole Analogues, Mohamed Jawed Ahsan
Turkish Journal of Chemistry
We report herein the synthesis, characterization, and cytotoxicity evaluations of some newer oxadiazole and triazole analogues (5a-j). The cytotoxicity of all the title compounds were evaluated as per the National Cancer Institute protocol in a one-dose assay (10 $\mu $M) on nine different panels of 59 cancer cell lines. 2-$\{$5-[(2,4-Dichlorophenoxy)methyl]-1,3,4-oxadiazol-2-yl$\}$phenol (5e) showed the maximum cytotoxicity among the series of ten compounds. The cytotoxicity of 5e was comparable to that of the standard anticancer drug, 5-fluorouracil, and better than that of imatinib. The structure activity relationship was also discussed.
Synthesis And Cytotoxicity Of Novel Thioxo-Quinazolino[3,4-$A$]Quinazolinones, Negar Mohammadhosseini, Mina Saeedi, Shahram Moradi, Mohammad Mahdavi, Omidreza Firuzi, Alireza Foroumadi, Abbas Shafiee
Synthesis And Cytotoxicity Of Novel Thioxo-Quinazolino[3,4-$A$]Quinazolinones, Negar Mohammadhosseini, Mina Saeedi, Shahram Moradi, Mohammad Mahdavi, Omidreza Firuzi, Alireza Foroumadi, Abbas Shafiee
Turkish Journal of Chemistry
Various thioxo-quinazolino[3,4-$a$]quinazolinones were prepared and evaluated for their cytotoxicity in MOLT-4 (lymphoblastic leukemia) and MCF-7 (breast adenocarcinoma) cell lines. Synthesis of the target compounds was started from isatoic anhydride. Successive reaction of isatoic anhydride with benzylamine and 2-nitrobenzaldehyde, reduction of the nitro group, and reaction with CS$_{2}$ gave 12-benzyl-6-thioxo-6,7,11b,12-tetrahydro-13$H$-quinazolino[3,4-$a$]quinazolin-13-one. The latter compound reacted with various 2-chloro-$N$-substituted acetamides to afford the corresponding fused quinazolinone derivatives.
Synthesis And Anticancer And Cytotoxic Effects Of Novel 1,4-Phenylene-Bis-N-Thiocarbamoylpyrazole And 1,4-Phenylene-Bis-Pyrazolylthiazole Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Yakup Budak, Ayşe Şahi̇n Yağlioğlu, Mustafa Ceylan
Synthesis And Anticancer And Cytotoxic Effects Of Novel 1,4-Phenylene-Bis-N-Thiocarbamoylpyrazole And 1,4-Phenylene-Bis-Pyrazolylthiazole Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Yakup Budak, Ayşe Şahi̇n Yağlioğlu, Mustafa Ceylan
Turkish Journal of Chemistry
Thiazolylpyrazoline derivatives were recently reported as potent anticancer agents. In this study, novel 1,4-phenylene-bis-N-thiocarbamoylpyrazoles (3a-h and 1,4-phenylene-bis-pyrazolylthiazoles (5a-h were prepared and screened for their anticancer activities against C6 (rat brain tumor cells) and HeLa (human uterus carcinoma). Anticancer activity studies were performed as a dose-dependent assay starting with eight concentrations. 5-Fluorouracil (5-FU) was used as a positive control. Compounds 3c, 3d, and 3h were examined and they revealed almost the same activities compared with 5-FU in terms of cell selectivity against C6 cells. Moreover, compounds 3a-h had lower cytotoxicity than 5-FU. The low cytotoxicity values of 3a-h as well as …
Synthesis Of Novel Thiazolylpyrazoline Derivatives And Evaluation Of Their Antimicrobial Activities And Cytotoxicities, Aouatef Tabbi, Zafer Asim Kaplancikli, Dahmane Tebbani, Leyla Yurttaş, Zerri̇n Cantürk, Özlem Atli, Merve Baysal, Gülhan Turan Zitouni
Synthesis Of Novel Thiazolylpyrazoline Derivatives And Evaluation Of Their Antimicrobial Activities And Cytotoxicities, Aouatef Tabbi, Zafer Asim Kaplancikli, Dahmane Tebbani, Leyla Yurttaş, Zerri̇n Cantürk, Özlem Atli, Merve Baysal, Gülhan Turan Zitouni
Turkish Journal of Chemistry
Several novel thiazolylpyrazoline derivatives were synthesized by reacting substituted 3,5-diaryl-1-thiocarba\-moyl-2-pyrazolines with phenacylbromides. The structures of the synthesized compounds were confirmed by IR, $^{1}$H NMR, $^{13}$C NMR, and MS spectral data. Their antimicrobial activities against Staphylococcus aureus(ATCC-25923), Enterococcus faecalis} (ATCC-29212), Enterococcus faecalis (ATCC-51922), Listeria monocytogenes (ATCC-1911), Klebsiella pneumoniae (ATCC-700603), Pseudomonas aeruginosa (ATCC-27853), Escherichia coli (ATCC-35218), Escherichia coli (ATCC-25922), Candida albicans (ATCC-90028), Candida glabrata (ATCC-90030), Candida krusei (ATCC-6258), and Candida parapsilosis (ATCC-22019) were investigated. The compounds were also studied for their cytotoxic effects using a MTT assay. Compound 7c showed the highest antimicrobial activity, possessing the same potential as chloramphenicol against K. …
Synthesis, Anticandidal Activity, And Cytotoxicity Of Some Thiazole Derivatives With Dithiocarbamate Side Chains, Leyla Yurttaş, Yusuf Özkay, Fati̇h Demi̇rci̇, Gamze Göger, Şafak Ulusoylar Yildirim, Usama Abu Mohsen, Ömer Öztürk, Zafer Asim Kaplancikli
Synthesis, Anticandidal Activity, And Cytotoxicity Of Some Thiazole Derivatives With Dithiocarbamate Side Chains, Leyla Yurttaş, Yusuf Özkay, Fati̇h Demi̇rci̇, Gamze Göger, Şafak Ulusoylar Yildirim, Usama Abu Mohsen, Ömer Öztürk, Zafer Asim Kaplancikli
Turkish Journal of Chemistry
Some thiazole derivatives bearing dithiocarbamic acid esters were synthesized in order to investigate their anticandidal activity and cytotoxicity. The structures of the obtained final compounds (6a--j) were confirmed by spectral data (IR, ^1H NMR, ^{13}C NMR, and MS) and elemental analysis. The anticandidal activity of the compounds was determined (6a--j) using the microbroth dilution method and their cytotoxicity was evaluated according to the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against normal cells. Contrary to expectations, weak antifungal activity was observed with IC_{50} values ranging between 30 and 403 \mu g/mL.
Design, Synthesis, And Biological Evaluation Of Indole-Based 1,4-Disubstituted Piperazines As Cytotoxic Agents, Meri̇ç Köksal Akkoç, Mi̇ne Yarim Yüksel, İrem Durmaz, Rengül Çeti̇n Atalay
Design, Synthesis, And Biological Evaluation Of Indole-Based 1,4-Disubstituted Piperazines As Cytotoxic Agents, Meri̇ç Köksal Akkoç, Mi̇ne Yarim Yüksel, İrem Durmaz, Rengül Çeti̇n Atalay
Turkish Journal of Chemistry
A series of 3-[(4-substitutedpiperazin-1-yl)methyl]-1H-indole derivatives were synthesized, and their structures were confirmed by spectral analysis. All the compounds were tested for their cytotoxic activity in vitro against 3 human tumor cell lines: human liver (HUH7), breast (MCF7), and colon (HCT116). Among the designed derivatives, most of the compounds showed significant cytotoxicity against liver and colon cancer cell lines with lower IC_{50} concentrations than the standard drug 5-fluorouracil. Compound 3s, with 3,4-dichlorophenyl substituent on the piperazine ring, was the most active in suppressing the growth of all screened cancer cells.
Synthesis Of New Bengazole Analogues And Their Antimicrobial Activity, Jurgen Krauss, Sandra Kalkbrenner, Angela Schuster, Anne Obainoke, Franz Bracher
Synthesis Of New Bengazole Analogues And Their Antimicrobial Activity, Jurgen Krauss, Sandra Kalkbrenner, Angela Schuster, Anne Obainoke, Franz Bracher
Turkish Journal of Chemistry
Bengazole A and bengazole B are 2 representatives out of a large family of marine metabolites isolated from a Jaspis sponge and display potent anti-fungal and anthelmintic activity as well as modest cytotoxic activity. This paper reports a short and efficient synthesis and microbiological evaluation of some new bengazole analogues.
Characterization And Antimicrobial Activity Of Organotin(Iv) Complexes Of 2-[(2´,6´-Diethylphenylamido)]Benzoates And 3-[(2´,6´-Diethylphenylamido)]Propanoates, Saira Shahzadi, Khadija Shahid, Saqib Ali, Mohammad Bakhtiar
Characterization And Antimicrobial Activity Of Organotin(Iv) Complexes Of 2-[(2´,6´-Diethylphenylamido)]Benzoates And 3-[(2´,6´-Diethylphenylamido)]Propanoates, Saira Shahzadi, Khadija Shahid, Saqib Ali, Mohammad Bakhtiar
Turkish Journal of Chemistry
New organotin(IV) complexes with 2-[(2',6'-diethylphenylamido)] benzoic acid (HL^1) and 3-[(2',6' -diethylphenylamido)]propanoic acid (HL^2) were synthesized by the reaction of di- and triorganotin salts in the presence of triethylamine as base or dioctyltin oxide using a Dean and Stark trap for the removal of azeotropic water. All complexes were characterized by elemental analysis, IR, NMR, and mass spectral studies, and proof that tin-ligand coordination involves only the carboxylate group and complexes show hexa-coordinated geometry in solid state. Multinuclear NMR data show that triorganotin complexes exhibit 4-coordinated geometry while diorganotin complexes show a coordination number greater than 4, probably 5 or 6 …
Synthesis, Spectroscopic And Biological Investigation Of Cyclic Octapeptide: Cherimolacyclopeptide G, Rajiv Dahiya
Synthesis, Spectroscopic And Biological Investigation Of Cyclic Octapeptide: Cherimolacyclopeptide G, Rajiv Dahiya
Turkish Journal of Chemistry
A natural cyclic octapeptide cherimolacyclopeptide G (8) was synthesized by coupling of tetrapeptide units Boc-Gly-Ala-Val-Pro-OMe (5) and Boc-Ile-Tyr-Ala-Pro-OMe (6) after proper deprotection at carboxyl and amino terminals followed by cyclization of the linear peptide segment. The structure was elucidated by IR, ^1H-NMR, ^{13}C-NMR, FAB MS spectral data, and elemental analyses. The newly synthesized cyclopeptide was also evaluated for its antimicrobial, anthelmintic, and cytotoxic activities and found to exhibit potent anthelmintic and cytotoxic activity against earthworms, Megascoplex konkanensis, Pontoscotex corethruses, and Eudrilus species, and Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines. In addition, compound 8 possessed moderate …
A New Approach To Furan-Containing Macrolactones, Christoph Schmidt, Ruth Messmer, Franz Bracher, Jurgen Krauss
A New Approach To Furan-Containing Macrolactones, Christoph Schmidt, Ruth Messmer, Franz Bracher, Jurgen Krauss
Turkish Journal of Chemistry
Furan and tetrahydrofuran heterocycles are part of many natural products, like the Galerucella pheromone, furano epothilones, bipinnatin, and amphidinolides. This paper describes a short and efficient synthetic approach to furan-containing macrolactones in 4 steps, including as key steps a Sonogashira reaction and an olefin metathesis. The resulting compounds were tested at the National Cancer Institute for their cytotoxicity, but did not exhibit significant cytotoxicity in the human tumour cell line screen.