Search results for "relationship"
showing 10 items of 3616 documents
1-methil-3H-pyrazolo[1-2-a]benzo[1-2-3-4]tetrazin-3-ones, design synthesis and biological activity of new antitumoral agents
2005
1-Methylpyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones 4, synthesized in good to excellent yields, were designed as novel alkylating agents because of their peculiar chemical behavior. All derivatives showed antiproliferative activity against more than 50 types of tumor cell lines with GI50 reaching sub-micromolar values. SAR studies revealed that the presence of a chlorine atom is well-tolerated in both positions 8 and 9, whereas in the case of the methyl group, switching from the 8 to the 9 position gives rise to the most active compound of the series, 4g, either for the number of cell lines inhibited and for selectivity against leukaemia and renal cancer subpanels. COMPARE and 3D-MIND comp…
3-(6-Phenylimidazo [2,1-
2019
A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increa…
Apmierinātības ar attiecībām saistība ar personības iezīmēm pāriem ar atšķirīgu attiecību ilgumu
2015
Pētījumā mērķis bija noskaidrot, kādas personības iezīmes ir nozīmīgi saistītas ar apmierinātību ar pāra attiecībām daţādās pāra attiecību ilguma grupās. Pētījumā piedalījās 115 pāri (230 respondenti), 39 pāri, kas pāra attiecībās ir 2 – 6 gadus, 38 pāri, kas pāra attiecībās ir 12 – 16 gadus un 38 pāri, kas pāra attiecībās ir 22 un vairāk gadus. Pētījumā tika izmantota Latvijas Personības aptauja (Perepjolkina & Reņģe, 2013), pašraksturojuma un citvērtējuma forma, un Apmierinātības ar attiecībām aptauja (/IMS/ - Index of Marital Satisfaction, Hudson & Walter, 1982). Pētījumā vīriešu un sieviešu izlasēs tika konstatētas nozīmīgas saistības starp apmierinātību ar pāra attiecībām un apzinīguma…
Understanding moderating effects in increasing share-of-wallet and word-of-mouth : A case study of Lidl grocery retailer
2018
This study examines how five moderating variables (the length of the customer relationship, following a company in print media and on social media, remembering online advertisements, and the customer’s age) affect the relationships between perceived value and loyalty and satisfaction and loyalty in the grocery retailing sector. A series of hypotheses were developed and tested with a sample of 2,072 discount retailer customers in Finland. The results support all the direct effects hypotheses and show that perceived value and satisfaction both have a positive effect on loyalty, measured as a share of wallet and word of mouth and that the effect of perceived value tends to be stronger in the s…
The valuable textbooks : a study on relationship values and attitudes in an EFL-textbook series
2010
Yksi yleissivistävän koulun tavoitteista on opettaa oppijoille arvoja ja asenteita. Nämä arvot ja asenteet näkyvät muun muassa opetussuunnitelmassa ja sitä myöten myös opetuskäytänteissä ja oppikirjoissa. Oppikirjatekstien välittämät arvot ja asenteet eivät ole kuitenkaan peräisin yksinomaan opetussuunnitelmassa lausutuista tavoitteista, vaan myös oppikirjantekijöiden maailmankuvat vaikuttavat niihin – joko tietoisesti tai tiedostamatta – teksteihin valittujen näkökulmien ja kielenkäytön kautta. Tässä tutkimuksessa selvitettiin millä tavoin lukion englannin oppikirjatekstit käsittelevät ja kuvaavat eri parisuhdemuotoja ja mitkä parisuhdearvot ja -asenteet vaikuttavat tekstien taustalla. Tut…
Los stages franceses. Tres claves para mejorar las prácticas para el empleo de los jóvenes en España
2016
El trabajo analiza, desde una perspectiva de Derecho comparado, los stages franceses o estancias de formación, que, en su acepción más estricta, son períodos de prácticas en empresas en educación universitaria. El Derecho francés mediante sucesivas reformas ha creado un estatuto de los stagiaires mediante el reconocimiento de una serie de derechos. Entre las idiosincrasias del Derecho francés, se instituye un derecho de gratificación cuando la duración es al menos de 2 meses y se limita la duración máxima del tiempo de prácticas aplicando los mismos topes de jornada de los trabajadores. El ordenamiento galo introduce limitaciones para evitar el uso desviado de estas prácticas no laborales c…
Evolution of Cell Adhesion Systems: Evidence for Arg-Gly-Asp-Mediated Adhesion in the Protozoan Neoparamoeba aestuarina
1995
Developmental processes in multicellular organisms require structural elements, such as adhesion molecules, to stabilize cells at functional positions. In vertebrates, a series of extracellular matrix proteins, e.g. fibronectin and laminin, are involved in cell adhesion. These proteins contain Arg-Gly-Asp [RGD] at their binding sites. Here we show that at concentrations above 2 mM the peptide GRGDSPK, comprising the tripeptide RGD (Arg-Gly-Asp), prevents the adhesiveness of cells of the marine amoeba Neoparamoeba aestuarina. In addition, elevated levels of GRGDSPK cause cells to alter their shapes from those with digitiform subpseudopodia to rounded cells with small lobed pseudopodia. These…
A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors.
2012
In this study we report the design, synthesis, and biological evaluation of constrained aminopyridinylimidazoles as p38α MAP kinase inhibitors. The frozen analogue approach focused on the pyridinyl unit, using purine bioisosteres as constrained structure analogues. The identification of the most potent bioisostere was followed by a further derivatization to address hydrophobic region II. In combination with C-2 modifications of the imidazole core, we were able to design highly active inhibitors on the p38α MAP kinase. The inhibitor design presented herein represents a promising and highly efficient advancement of recent stages of development in this class of p38 MAP kinase inhibitors. In co…
Theoretical studies of HIV-1 reverse transcriptase inhibition
2012
Computational methods for accurately calculating the binding affinity of a ligand for a protein play a pivotal role in rational drug design. We herein present a theoretical study of the binding of five different ligands to one of the proteins responsible for the human immunodeficiency virus type 1 (HIV-1) cycle replication; the HIV-1 reverse transcriptase (RT). Two types of approaches are used based on molecular dynamics (MD) simulations within hybrid QM/MM potentials: the alchemical free energy perturbation method, FEP, and the pathway method, in which the ligand is physically pulled away from the binding site, thus rendering a potential of mean force (PMF) for the binding process. Our com…
In vitro enterococcus faecalis biofilm formation on five adhesive systems
2011
Objective: To determine the E. faecalis biofilm formation on the surface of five adhesive systems (AS) and its relationship with roughness. Study Design: The formation of E. faecalis biofilms was tested on the surface of four dual-cure AS: AdheSE DC, Clearfil DC Bond, Futurabond DC and Excite DSC and one light-cure antimicrobial AS, Clearfil Protect Bond, after 24 hours of incubation, using the MBEC high-throughput device. Results: E. faecalis biofilms grew on all the adhesives. The least growth of biofilm was on Excite DSC, Clearfil Protect Bond, and the control. Futurabond DC resulted in the greatest roughness and biofilm amount. There was a close relationship between the quantity of biof…