Search results for "IPR"
showing 10 items of 1515 documents
Sistemas electrónicos para el tratamiento de la información (2010/2011)
2010
Imidazo[2,1-b] [1,3,4]thiadiazoles with antiproliferative activity against primary and gemcitabine-resistant pancreatic cancer cells
2020
A new series of eighteen imidazo [2,1-b] [1,3,4]thiadiazole derivatives was efficiently synthesized and screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. Two out of eighteen derivatives, compounds 12a and 12h, showed remarkably cytotoxic activity with the half maximal inhibitory concentration values (IC50) ranging from 0.23 to 11.4 μM, and 0.29–12.2 μM, respectively. However, two additional compounds, 12b and 13g, displayed remarkable in vitro antiproliferative activity against pancreatic ductal adenocarcinoma (PDAC) cell lines, including immortalized (SUIT-2, Capan-1, Panc-1), primary (PDAC-3) and gemcitabine-resistant (Panc-1R), elici…
Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.
2015
Novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation were developed; some of them possess K(i) values in the micromolar range. We studied the structure-activity relationship of these derivatives and we performed docking studies, which allowed us to find out the key interactions established by the inhibitors with the target enzyme. Biological results indicate that the nature of the P2 and P3 substituents and their binding to the S2/S3 pockets is strictly interdependent.
Lipoprotein-induced phenoloxidase-activity in tarantula hemocyanin.
2015
Phenoloxidases play vital roles in invertebrate innate immune reactions, wound closure and sclerotization processes in arthropods. In chelicerates, where phenoloxidases are lacking, phenoloxidase-activity can be induced in the oxygen carrier hemocyanin in vitro by proteolytic cleavage, incubation with the artificial inducer SDS, or lipids. The role of protein-protein interaction has up to now received little attention. This is remarkable, as lipoproteins - complexes of proteins and lipids - are present at high concentrations in arthropod hemolymph. We characterized the three lipoproteins present in tarantula hemolymph, two high-density lipoproteins and one very high-density lipoprotein, and…
El método del caso como herramienta de aprendizaje activo en arqueología
2021
[EN] The case study, like other methodologies that enhance the active participation of the students, greatly favours the teaching-learning process. Here we present the design, application and results of the cases implemented in two Archaeology subjects (History Degree, University of Valencia). Within the framework of a Teaching Innovation Project (METARQ), we have implemented, in six different groups, two cases related to two subjects: Archaeological Methodology (3rd year-2nd semester, three groups) and Mediterranean Archaeology (4th year-1st semester, three groups). Both the learning results and the general opinion of the students were very positive. In addition, the application of this po…
Rational Design of Single-Ion Magnets and Spin Qubits Based on Mononuclear Lanthanoid Complexes
2012
Here we develop a general approach to calculating the energy spectrum and the wave functions of the low-lying magnetic levels of a lanthanoid ion submitted to the crystal field created by the surrounding ligands. This model allows us to propose general criteria for the rational design of new mononuclear lanthanoid complexes behaving as single-molecule magnets (SMMs) or acting as robust spin qubits. Three typical environments exhibited by these metal complexes are considered, namely, (a) square antiprism, (b) triangular dodecahedron, and (c) trigonal prism. The developed model is used to explain the properties of some representative examples showing these geometries. Key questions in this ar…
Multibiomarker approach to fipronil exposure in the fish Dicentrarchus labrax under two temperature regimes
2020
12 pages, 5 figures, 3 tables, supplementary data https://doi.org/10.1016/j.aquatox.2019.105378
Highly Efficient Removal of Neonicotinoid Insecticides by Thioether-Based (Multivariate) Metal–Organic Frameworks
2021
Circumventing the impact of agrochemicals on aquatic environments has become a necessity for health and ecological reasons. Herein, we report the use of a family of five eco-friendly water-stable isoreticular metal-organic frameworks (MOFs), prepared from amino acids, as adsorbents for the removal of neonicotinoid insecticides (thiamethoxam, clothianidin, imidacloprid, acetamiprid, and thiacloprid) from water. Among them, the three MOFs containing thioether-based residues show remarkable removal efficiency. In particular, the novel multivariate MOF {SrIICuII6[(S,S)-methox]1.5[(S,S)-Mecysmox]1.50(OH)2(H2O)}·36H2O (5), featuring narrow functional channels decorated with both -CH2SCH3 and -CH2…
Efficacy of an insecticide paint against malaria vectors and nuisance in West Africa--part 2: field evaluation.
2010
Abstract Background Widespread resistance of the main malaria vector Anopheles gambiae to pyrethroids reported in many African countries and operational drawbacks to current IRS methods suggest the convenience of exploring new products and approaches for vector control. Insecticide paint Inesfly 5A IGR™, containing two organophosphates (OPs), chlorpyrifos and diazinon, and one insect growth regulator (IGR), pyriproxyfen, was tested in Benin, West Africa, for 12 months. Methods Field trials were conducted in six experimental huts that were randomly allocated to one or two layers of insecticide at 1 Kg/6 m2 or control. Evaluations included: (i) early mosquito collection, (ii) mosquito release…
A new lattice action for studying topological charge
1996
We propose a new lattice action for non-abelian gauge theories, which will reduce short-range lattice artifacts in the computation of the topological susceptibility. The standard Wilson action is replaced by the Wilson action of a gauge covariant interpolation of the original fields to a finer lattice. If the latter is fine enough, the action of all configurations with non-zero topological charge will satisfy the continuum bound. As a simpler example we consider the $O(3)$ $\sigma$-model in two dimensions, where a numerical analysis of discretized continuum instantons indicates that a finer lattice with half the lattice spacing of the original is enough to satisfy the continuum bound.