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Taste, A New Incentive to Switch to (R)-Praziquantel in Schistosomiasis Treatment
The schistosomicidal component alone of (R)-PZQ is significantly less bitter than regular, racemic PZQ, and should be specifically suitable for the treatment of school-age children againstschistosomiasis. Expand
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
The pyrrole-2-one moiety was dissected from the corresponding maleimide protein kinase inhibitor as a suitable key pharmacophore and found to possess highly potent antiangiogenic activities in the cellular HLMEC sprouting assay and also slightly induced apoptosis in HDMECs whereas 3 was determined to be significantly less active. Expand
Inhibitors of Inducible NO Synthase Expression: Total Synthesis of (S)‐Curvularin and Its Ring Homologues
In the evaluation of the anti‐inflammatory effects of the synthesized compounds in assays using cells stably transfected with a human iNOS promoter–luciferase reporter gene construct, the 14‐ and 16‐membered homologues showed a slightly higher inhibitory effect towards iN OS promoter activity than curvularin itself. Expand
Characterization of the synthetic cannabinoid MDMB-CHMCZCA
The synthetic cannabinoid MDMB-CHMCZCA was characterized by various spectroscopic techniques including NMR spectroscopy and tandem mass spectrometry and the enantiomeric purity of samples from test purchases and police seizures was assessed by a self-developed chiral HPLC method. Expand
Structure determination by electron crystallography using both maximum-entropy and simulation approaches
Ab initio structure determination and refinement from electron diffraction data is not a widely used technique in structural science because of the inaccuracies inherent in the process of intensityExpand
X-ray diffraction analysis of butyl- and isobornyl acrylate/heptakis(2,6-di-O-methyl)-β-cyclodextrin complexes and correlation to 1H NMR-spectra
The crystal structures of the complexes n-butyl acrylate/heptakis(2,6-di-O-methyl)-β-cyclodextrin and isobornyl acrylate/heptakis(2,6-di-O-methyl)-β-cyclodextrin were investigated by X-rayExpand
Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
Structural-activity relationships (SAR) relationships for this compound series with the isolated enzyme and equivalent antiangiogenic activity in the chick embryo assay are presented herein. Expand
Synthesis and cytotoxicity of 6,11-dihydro-pyrido- and 6,11-dihydro-benzo[2,3-b]phenazine-6,11-dione derivatives.
The study on the cytotoxicity on these products revealed that the pyridophenazinediones, tetracyclic heteroquinone analogues with three nitrogen atoms exhibited a high cytot toxicity on several human tumor cell lines. Expand
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.
By comparing the X-ray structures of the compounds, it is found a significantly larger distance between the pyridine and the 4-F-phenyl moiety in five-membered core structures relevant for ligand-protein interactions. Expand
Columnar supramolecular architecture of crystals of 2-(4-Iodophenyl)-1,10-phenanthroline derived from values of intermolecular interaction energy
Using results of X-ray diffraction study supramolecular architecture of crystals of 2-(4-iodophenyl)-1,10-phenanthroline has been analyzed on the basis of quantum-chemical calculations ofExpand