Bioactivity focus on α-cyano-4-hydroxycinnamic acid (CHCA) scaffold results in a small library of novel multifunctional aldose reductase (ALR2) inhibitors. All the entities displayed good to excellent inhibition with IC50 72-405 nM. (R,E)-N-(3-(2-acetamido-3-(benzyloxy)propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (5f) was confirmed as the most active inhibitor (IC50 72.7 ± 1.6 nM)...

African trypanosomes are capable of both pyrimidine biosynthesis and salvage of preformed pyrimidines from the host. However, uptake of pyrimidines in bloodstream form trypanosomes has not been investigated, making it difficult to judge the relative importance of salvage and synthesis or to design a pyrimidine-based chemotherapy. Detailed characterization of pyrimidine transport activities in b...

A dramatic temperature dependent enhancement of U 5f spectral weight at EF is observed in angle-resolved photoemission measurements of URu2Si2 at the center of an X-point hole-pocket. Comparison of this temperature dependent behavior for excitation both at and below the U 5d→5f resonant threshold is presented.

The 5- and 6-fluoro derivatives of arachidonic acid (5F-ETE and 6F-ETE) were evaluated as substrates of rat basophilic leukaemia cell (RBL-1) 5-lipoxygenase. 5F-ETE was found to be a poor substrate and was converted into a single product, 5-oxoeicosa-6,8,11,14-tetraenoic acid (5-oxo-ETE). 6F-ETE was a good substrate and was mainly converted into 5-hydroperoxy-6-fluoroeicosa-6,8,11,14-tetraenoic...

Background: Radiation-induced lung injury is a refractory side effect in lung cancer radiotherapy, the mechanism still remains unclear, hence an appropriate animal mode may become useful to investigate it. Materials and Methods: 50 female Wistar rats were randomly divided into 5 groups, average 10 rats/cage: A. control group B. 3Gy×10f C. 6Gy×5f D. 12.5Gy×1f E.15.3Gy×1f....

Systematic trends in the results of magnetic and specific-heat studies of UTX compounds (T = transition metal, X = p element) are discussed in terms of the degree of the U-Sf electron delocalization which is controlled by the strength of 5f-ligand hybridization. Continuous changes of this parameter and its influence on ground-state properties were investigated in solid solutions of selected UTX...

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The ground and excited states of the UO(2) molecule have been studied using a Dirac-Coulomb intermediate Hamiltonian Fock-space coupled cluster approach (DC-IHFSCC). This method is unique in describing dynamic and nondynamic correlation energies at relatively low computational cost. Spin-orbit coupling effects have been fully included by utilizing the four-component Dirac-Coulomb Hamiltonian fr...

An understanding of the phase diagram of elemental plutonium (Pu) must include both, the effects of the strong directional bonding and the high density of states of the Pu 5f electrons, as well as how that bonding weakens under the influence of strong electronic correlations. Here we present electronic-structure calculations of the full 16-atom per unit cell α-phase structure within the framewo...