Search results for "Screen"
showing 10 items of 1374 documents
Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.
2015
Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptos…
Synchronizing the release rates of salicylate and indomethacin from degradable chitosan hydrogel and its optimization by definitive screening design.
2018
Abstract Three types of ionically crosslinked (with citric acid) chitosan discs were loaded with the highly water- soluble drug, sodium salicylate (SS) and the poorly water-soluble drug, indomethacin (Ind). In separate experiments the hydrated discs were immersed in a de-crosslinking solution comprising of different concentrations of calcium chloride, which induced a controlled erosion of the discs, a process which was optimized to synchronize the release rates of the two drugs over a predetermined period of time. The optimization was accomplished by manipulating six factors: chitosan MW, its amount in the formulation, the concentration of the crosslinker agent, the concentration of the de-…
A dual process model to predict adolescents’ screen time and physical activity
2021
OBJECTIVE: Many adolescents report a lack of physical activity (PA) and excess screen time (ST). Psychological theories aiming to understand these behaviours typically focus on predictors of only one behaviour. Yet, behaviour enactment is often a choice between options. This study sought to examine predictors of PA and ST in a single model. Variables were drawn from dual process models, which portray behaviour as the outcome of deliberative and automatic processes. DESIGN: 411 Finnish vocational school students (age 17-19) completed a survey, comprising variables from the Reasoned Action Approach (RAA) and automaticity pertaining to PA and ST, and self-reported PA and ST four weeks later. M…
Construcción y validación de un sistema de detección precoz de trastornos de desarrollo (SDPTD) en niños de 18, 24, y 36 meses
2013
En esta tesis se pretende contruir una herramienta de detección precoz que detecte cualquier alteración que se produzca en el desarrollo del niño como una medida preventiva de posibles trastornos posteriores más graves. En esta investigación se ha diseñado una herramienta basada en web y apoyada en videos para facilitar a las familias la administración. El sistema esta compuesto de 7 cuestionarios pero en esta tesis estan validados los 3 cuestionarios (18 meses, 24 meses y 36 meses). Los cuestionarios se pueden encontrar en: https://cudap.uv.es/ProyectoC/
Efficacy of an internet-based psychological intervention for problem gambling and gambling disorder: study protocol for a randomized controlled trial
2021
Gambling Disorder is a prevalent non-substance use disorder, which contrasts with the low number of people requesting treatment. Information and Communication Technologies (ICT) could help to enhance the dissemination of evidence-based treatments and considerably reduce the costs. The current study seeks to assess the efficacy of an online psychological intervention for people suffering from gambling problems in Spain. The proposed study will be a two-arm, parallel-group, randomized controlled trial. A total of 134 participants (problem and pathological gamblers) will be randomly allocated to a waiting list control group (N = 67) or an intervention group (N = 67). The intervention program i…
The lignan, (-)-sesamin reveals cytotoxicity toward cancer cells: pharmacogenomic determination of genes associated with sensitivity or resistance.
2013
(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. Multidrug resistance (MDR) of tumors leads to fatal treatment outcome in many patients and novel drugs able to kill multidrug-resistant cells are urgently needed. P-glycoprotein (MDR1/ABCB1) is the best known ATP-binding cassette (ABC) drug transporter mediating MDR. ABCB5 is a close relative to ABCB1, which also mediates MDR. We found that the mRNA expressions of ABCB1 and ABCB5 were not related to the 50% inhibi…
Binding mode analysis of ABCA7 for the prediction of novel Alzheimer's disease therapeutics
2021
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Genetic determinants of ATR inhibitor sensitivity and resistance in Gastric Cancer
2019
Synthetic lethal approaches in identifying genetic determinants of drug response is a powerful method in selecting patents for targeted cancer therapies. Ataxia-Telangiectasia Mutated (ATM) and Rad3-related protein kinase (ATR) is a valuable target to inhibit the DNA damage repair (DDR) pathway, that has been shown to be particularly effective in cancer cells harbouring other DDR defects, including truncating mutations in ARID1A, found in the 20% of gastric cancer (GC) patients. Although ATR inhibitors (ATRi) are emerging as promising cancer therapies, resistance mechanisms inevitably arise from these drugs as monotherapy, emphasising the importance of identifying genetic determinants of re…
Estimation of ADME Properties in Drug Discovery: Predicting Caco-2 Cell Permeability Using Atom-Based Stochastic and Non-stochastic Linear Indices
2007
The in vitro determination of the permeability through cultured Caco-2 cells is the most often-used in vitro model for drug absorption. In this report, we use the largest data set of measured P(Caco-2), consisting of 157 structurally diverse compounds. Linear discriminant analysis (LDA) was used to obtain quantitative models that discriminate higher absorption compounds from those with moderate-poorer absorption. The best LDA model has an accuracy of 90.58% and 84.21% for training and test set. The percentage of good correlation, in the virtual screening of 241 drugs with the reported values of the percentage of human intestinal absorption (HIA), was greater than 81%. In addition, multiple …
Cladosins L-O, new hybrid polyketides from the endophytic fungus Cladosporium sphaerospermum WBS017
2019
Abstract The endophytic fungus Cladosporium sphaerospermum WBS017 was obtained from healthy bulbs of Fritillaria unibracteata var. wabuensis. Fermentation of C. sphaerospermum on solid rice medium yielded three new hybrid polyketides, cladosins L−N (1–3), and a known derivative cladodionen (4). Further cultivation of this fungus on white bean medium afforded an additional new hybrid polyketide, cladosin O (5) along with three known analogues (6–8). The structures of the new compounds were elucidated using a combination of NMR and HRESIMS data. The absolute configurations of compounds 2 and 3 were determined by Mosher’s method and TDDFT-ECD calculations. All isolated compounds were evaluated…