Design, synthesis, and biological evaluation of indole-based 1,4-disubstituted piperazines as cytotoxic agents

Köksal, Meriç Akkoc | Yarım, Mine Yüksel | Durmaz, İrem | Çetin, Rengül Atalay

Article | 2012 | Turkish Journal of Chemistry36 ( 4 ) , pp.503 - 514

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 IC50 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 Daha fazlası Daha az

Linear assembly and 3D networks of peptide modified gold nanoparticles

Kalay, Saban | Blanchet, Clement | Culha, Mustafa

Article | 2014 | Turkish Journal of Chemistry38 ( 5 ) , pp.686 - 700

The charge and size of molecules chemically attached to nanoparticles (NPs) play an important role in their interaction behavior in suspensions. Gold nanoparticles (AuNPs) were modified systematically with peptides and the modification was verified with surface-enhanced Raman scattering (SERS). The behavior of the modified AuNPs in suspension and at the liquidsolid interface was monitored using small angle X-ray scattering (SAXS), UV/Vis spectroscopy and dynamic light scattering (DLS) in suspension, and atomic force microscopy (AFM) at the solid liquid interface. It was found that while negatively charged peptide modified AuNPs beha . . .ve very similar to citrate reduced AuNPs due to their negatively charged surface, positively charged peptide modified AuNPs showed significantly different assembly/aggregation properties in suspension. The formation of linear assemblies of positively charged peptide (CKRHSKRHRSKRHSKRHSKRHSKR) modified AuNPs was clearly observed from the AFM analysis of the droplet areas of its colloidal suspension. The combined analyses of data obtained from the employed techniques suggest that the positively charged large peptide modified AuNPs can form linear and 3D-like networks in the suspension. This study reveals important information regarding the surface property dependent behavior of NPs that may help in efforts to build higher structures using NPs as building blocks Daha fazlası Daha az

Neural Network Based Classification of Melanocytic Lesions in Dermoscopy: Role of Input Vector Encoding

Ertaş, Gökhan

Article | 2018 | Electrica18 ( 2 ) , pp.242 - 248

Melanocytic lesions are the main cause of death from skin cancer, and early diagnosis is the key to decreasing the mortality rate. This studyassesses the role of input-vector encoding in neural network-based classification of melanocytic lesions in dermoscopy. Twelve dermoscopicmeasures from 200 melanocytic lesions are encoded by compact encoding, ACD encoding, 1-of-N encoding, normalized encoding, and rawencoding, resulting in five different input-vector sets. Feed-forward neural networks with one hidden layer and one output layer are designedwith several neurons in the hidden layer, ranging from two to twenty-two for each type of . . .input-vector set, to classify a melanocytic lesion intocommon nevus, atypical nevus, and melanoma. Accordingly, 105 networks are designed and trained using supervised learning and then testedby performing a 10-fold cross validation. All the neural networks achieve high sensitivities, specificities, and accuracies in classification. However,the network with seven neurons in the hidden layer and raw encoded dermoscopic measures as the input vector realizes the highest sensitivity(97.0%), specificity (98.1%), and accuracy (98.0%). The practical use of the network can facilitate lesion classification by retaining the neededexpertise and minimizing diagnostic variability among dermatologists Daha fazlası Daha az

Energy savings in simultaneous multi-threaded processors through dynamic resizing of datapath resources

Küçük, Gürhan | Mesta, Mine

Article | 2012 | Turkish Journal of Electrical Engineering and Computer Sciences20 ( 1 ) , pp.125 - 139

Nowadays, all the designers of systems from high-performance servers to battery-operated handheld devices aim for reliability, high-performance and longevity. Central within these aims the issue of processor power consumption is becoming increasingly important. In this study, we aim to adapt our already-provenmethod for single-threaded superscalar processors to simultaneous multi-threaded (SMT) processors for energy savings. The original method focused on resizing datapath resources according to the demands of running applications. To achieve this, the targeted resources are physically divided into multiple partitions, and turned on . . . and off according to the needs of the applications. Since, the energy consumption of the turned-off datapath resources is quite low, as a result, it becomes possible to have great amount of energy savings within a processor. However, special care must be taken when there are multiple threads racing against each other to gain access to shared datapath resources. As a result, our proposed microarchitectural technique achieves 0.5% Instructions Per Cycle (IPC) and 3.2% Total number of instructions Per Cycle (TPC) improvement, while it turns off 45% of the Reorder Buffer (ROB), 59% of the Load-Store Queue (LSQ), 43% of the Issue Queue (IQ), 30% of the integer Physical Register Files (PRF) and, finally, 48% of the floating PRF, on the average across all simulated benchmarks. According to our estimates, the total processor power is reduced by 12%, on the average Daha fazlası Daha az

Mannich base derivatives of 3-hydroxy-6-methyl-4H-pyran-4-one with antimicrobial activity

Us, Demet | Berk, Barkın | Gürdal, Ece | Aytekın, Nihan | Kocagöz, Tanıl | Layan, Berrak Çağ | Erol, Dilek Demir

Article | 2010 | Turkish Journal of Chemistry34 ( 3 ) , pp.447 - 456

A series of 3-hydroxy-6-methyl-2-[(substitutedpiperidine-1-yl)methyl]-4H -pyran-4-one structured compounds were synthesized by reacting 5-hydroxy-2-methyl-4H -pyran-4-one with suitable piperidine derivatives using Mannich reaction conditions. Antibacterial activities of the compounds for E. coli ATCC 25922, S. paratyphi ATCC BAA-1250, S. flexneri ATCC 12022, E. gergoviae ATCC 33426, and M. smegmatis ATCC 14468 were assessed in vitro by the broth dilution method for determination of minimum inhibitory concentration (MIC). In addition, their inhibitory effects over DNA gyrase enzyme were evaluated using a DNA gyrase supercoiling assay . . .. All the synthesized compounds showed a MIC value of either 8 or 16 μg/mL for M. smegmatis, whereas minimum to moderate activity was achieved for the others. Those tested in the supercoiling assay had at best a very mild inhibition of the enzyme. This series deserves further attention for testing over Mycobacterium species and topoisomerase II inhibition to develop new lead drugs to treat non-tuberculous mycobacterial infections Daha fazlası Daha az

Fundamental noise studies in flame atomic magneto-optic rotation and atomic absorption spectrometry

İnce, Ahmet T. | Snook, Richard D. | Dawson, John B.

Other | 2000 | Turkish Journal of Chemistry24 ( 1 ) , pp.43 - 58

A study of inherent noise sources present in a purpose built flame atomic magneto-optic rotation (AMOR) spectrometer system was carried out with a view to identifying their sources. Two different optical configurations were employed, a crossed polariser and a 45° offset polariser configuration. The offset polariser configuration was operated in both an AMOR and atomic absorption (AA) mode for the noise measurements. Two main interference frequencies were found to occur in all the optical measurement modes. An interference flame feature frequency (15.5 Hz -39.0 Hz) which arose from an "organ-pipe" effect in the gas flow . . . through the flame cooling sheets. The second interference frequency (at 100 Hz) was thought, to arise due to modulation of the analytes magneto-optic properties due to ripple on the electromagnet d.c. power supply. Photon noise and fluctuation noise were found to be present as background noise. The fluctuation noise was dominant at. higher analyte concentrations. The characteristics and origins of fluctuation noise are discussed and investigated for each measurement mode. The noise spectra of the conventional AA measurements were compared with those of the contemporary AMOR measurements, to ascertain any differences in noise power spectra which may affect, the signal-to-noise ratio Daha fazlası Daha az

Design, optimization, and realization of a wire antenna with a 25:1 bandwidth ratio for terrestrial communications

Yeğin, Korkut

Article | 2014 | Turkish Journal of Electrical Engineering and Computer Sciences22 ( 2 ) , pp.371 - 379

Wire antennas can be made wideband if the antenna is loaded with passive elements and connected to a lossless matching network. However, realization of the load component values and matching network can easily become impractical. In this study, using only a surface mount and standard component values, antenna loads and a matching network are optimized using genetic algorithms. The optimized design achieves a 25:1 bandwidth ratio, from 20 MHz to 500 MHz, with a maximum voltage standing wave ratio (VSWR) of 3.5 and minimum system gain of --5 dBi. The antenna system gain at azimuth is taken as the objective function and an exact penalt . . .y function is formulated to take into account the VSWR over the design frequency band. A loaded antenna is built and measured to corroborate the simulations results. The realized antenna is only 0.14 lambda long at 20 MHz Daha fazlası Daha az

Dynamics, stability, and actuation methods for powered compass gait walkers

Şafak, Koray Kadir

Article | 2014 | Turkish Journal of Electrical Engineering and Computer Sciences22 ( 6 ) , pp.1611 - 1624

In this paper, methods to achieve actively powered walking on level ground using a simple 2-dimensional walking model (compass-gait walker) are explored. The walker consists of 2 massless legs connected at the hip joint, a point mass at the hip, and an infinitesimal point mass at the feet. The walker is actuated either by applying equal joint torques at the hip and ankle, by an impulse applied at the toe off, immediately before the heel strike, or by the combination of both. It is shown that actuating the walker by equal joint torques at the hip and ankle on level ground is equivalent to the dynamics of the passive walker on a downh . . .ill slope. The gait cycle for the simplified walker model is determined analytically for a given initial stance angle. Stability of the gait cycle by an analytical approximation to the Jacobian of the walking map is calculated. The results indicate that the short-period cycle always has an unstable eigenvalue, whereas stability of the long-period cycle depends on selection of the initial stance angle. The effect of the torso mass by adding a third link attached at the hip joint is investigated. The torso link is kept in the vertical position by controlling the torque applied to it. The proportional-derivative control law is utilized to regulate the angular position error of the torso link. Using linearized dynamics for this walker, active control is applied to the ankle, which reduces the dynamics of the walker to the passive walker without the torso. The proposed walker is capable of producing stable walking while keeping the torso in an upright positio Daha fazlası Daha az

Weak penetration and radiation through apertures in conducting bodies of revolution

Yeğin, Korkut

Article | 2009 | Turkish Journal of Electrical Engineering and Computer Sciences17 ( 3 ) , pp.231 - 239

The simplest way to solve for penetration through small apertures in conducting surfaces is to treat the body as a scatterer and determine the interior field as the sum of the incident field and the scattered field contributed by the current induced on the surface of the body. However, it is well known that, if the aperture is very small or if the penetrated field is very weak this method yields very inaccurate results, which, in turn, prohibits proper design of electronic systems, especially for electromagnetic compatibility and interference. Previously, alternative integral equations formulations were proposed to remedy this probl . . .em and applied to two-dimensional conducting cylinders with slots [1–2]. Application of these alternative techniques to threedimensional conducting bodies of revolution (BOR) is studied in this work. In addition, the reciprocity principle is used to recast a weak penetration problem into a weak radiation problem, and it is shown that the alternative formulations useful for weak penetration are also useful for weak radiation. The important features and relative accuracies of each formulation together with numerical results are detailed for mock missile-shape structures Daha fazlası Daha az

4H-Pyran-4-one derivatives:; leading molecule for preparation of compounds with antimycobacterial potential

Us, Demet | Gürdal, Ece | Berk, Barkın | Öktem, Sinem | Kocagöz, Tanıl | Çağlayan, Berrak | Erol, Dilek Demir

Article | 2009 | Turkish Journal of Chemistry33 ( 6 ) , pp.803 - 812

A series of 3-hydroxy-6-methyl-2-((4-substitutedpiperazin-1-yl)methyl)-4H-pyran-4-one structured compounds were synthesized by reacting 5-hydroxy-2-methyl-4H-pyran-4-one with suitable piperazine derivatives using Mannich reaction conditions. Antibacterial activities of the compounds for E. coli, S. paratyphi, S. flexneri, E. gergoviae, and M. smegmatis were assessed in vitro by using broth dilution for determination of the minimum inhibitory concentration (MIC). In addition, their inhibitory effects over DNA gyrase enzyme were evaluated using a DNA gyrase supercoiling assay. Among the synthesized compounds; compound 7 showed a 4 &am . . .p;#956;g/mL MIC value for M. smegmatis, whereas the other compounds demonstrated moderate to high activity. Those tested in the supercoiling assay had at best a very mild inhibition of the enzyme. This series deserves further attention for testing over Mycobacterium species and topoisomerase II inhibition to develop new lead drugs Daha fazlası Daha az


Utku, Feride Sermin | Basaran, Kubra | Sunar, Yagmur | Celebıoglu, Hulya | Kapıcı, Ibrahim

Article | 2017 | Istanbul University Journal of Electrical and Electronics Engineering17 ( 2 ) , pp.3439 - 3443

Mineralized natural protein based novel bone replacement materials are investigated for tissue engineering. Mineralized silk fibroin composite foams and films display excellent biocompatibility. In this study, the biomimetic and electrochemical mineralization of orderly oriented silk fibroin scaffolds was studied. Commercially obtained pure silk woven fabric was boiled in 0.02 M Na2CO3 for 20 min. Calcium phosphate was deposited at 37°C for twenty minutes in seven sequential immersion steps, using 250 mM CaCl2 2H2O and 120 mM K2HPO4, containing 0.15 M NaCl and 50mM TRIS-HCl, pH 7.4, followed by electrochemical treatment in modif . . .ied SBF solution at 40°C at a current density of -25mA/cm2 for 60 min. The amount of biomimetically deposited Ca-P increased with the number of immersion steps. SEM images and XRD analysis of the Ca-P deposit indicated the initial formation of brushite with its monoclinic crystal structure and characteristic peak at 11.76 2?, and electrochemical conversion of brushite to hydroxyapatite on silk after electrochemical cathodization as confirmed by XRD and SEM analysis. Thus, a silk-fibroin-hydroxyapatite composite material prepared as a xenograft consisting of biocompatible components, and easily prepared as an economical bone segment replacement material with highly oriented fibers Daha fazlası Daha az

Some new Mannich bases of 5-methyl-2-benzoxazolinones with analgesis and anti-inflammatory activities

Gökhan, Nesrin | Köksal, Meriç | Küpeli, Esra | Yeşilada, Erdem | Erdoğan, Hakkı

Article | 2005 | Turkish Journal of Chemistry29 ( 4 ) , pp.445 - 454

The synthesis of a novel series of Mannich bases of 5-methyl-3-substituted piperazinomethyl-2-benzoxazolinones is described. The structures attributed to compounds 3c, 3d and 3f-3n were elucidated using IR and 1H NMR spectroscopic techniques as well as elemental analysis. The compounds were examined for their in vivo anti-inflammatory and analgesic activities in 2 different bioassays, namely, carrageenan-induced hind paw edema and p-benzoquinone-induced abdominal constriction tests in mice, respectively. In addition, the ulcerogenic effects of the compounds were determined. Among the derivatives tested the most promising results wer . . .e obtained for the compounds bearing electron-withdrawing substituents (F, Cl, COCH_3) in the para position of the phenyl nucleus on the piperazine ring at the 3 position of benzoxazolinone moiety (3a, 3c, 3i). The analgesic activities of all compounds are higher than their anti-inflammatory activities and therefore these high analgesic activities indicated that the compounds could a show central effect Daha fazlası Daha az

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