Insulin-like growth factor-1 receptor (IGF-1R) is a growth factor receptor tyrosine kinase acting as a critical mediator of cell proliferation and survival. Novel 5-benzylidenethiazolidine-2,4-dione (5) and 5-(furan-2-ylmethylene)thiazolidine-2,4-dione (6) compounds were identified as potent and selective IGF-1R inhibitors via hierarchical virtual screening. Initial SAR and biological activity ...

The localization and some characteristics of mouse adrenal C19-steroid 5fi-reductase were determined by the incubation of subcellular fractions of mouse adrenal tissue with [7a-3H]androst-4-ene-3,17-dione. This enzyme was present only in the soluble fraction and was NADPH-dependent, although a small activity in the presence ofNADH was also detected. The soluble fraction also contained 3 a-, 3,6...

An inferred ancient episode of heating and deformation on Tethys has been attributed to its passage through a 3:2 resonance with Dione (Chen, E.M.A., Nimmo, F. [2008]. Geophys. Res. Lett. 35, 19203). The satellites encounter, and are trapped into, the e-Dione resonance before reaching the e-Tethys resonance, limiting the degree to which Tethys is tidally heated. However, for an initial Dione ec...

3-Ketosteroid-∆1-dehydrogenase (KstD), a key enzyme in microbial steroid catabolism, catalyzes the trans-axial elimination of the C1 and C2 hydrogen atoms of the A-ring from the polycyclic ring structure of 3-ketosteroids, and it was usually used to transform androst-4-ene-3,17-dione (AD) to produce androsta-1,4-diene-3,17-dione. Here, the KstD from Gordonia neofelifaecis was expressed efficien...

The lipophilicity of a series of Schiff base ligands and their complexes with nickel(II) and copper(II) has been determined by reversed-phase thin-layer chromatography using binary dioxane-water mobile phase. Chelate ligands were prepared by condensation of diamine and the corresponding beta-diketone. Copper(II) and nickel(II) complexes with chelate ligands containing ethane-1,2-diamine or prop...

Five new diketopiperazine derivatives, (3Z,6E)-1-N-methyl-3-benzylidene-6-(2S-methyl-3-hydroxypropylidene)piperazine-2,5-dione (1), (3Z,6E)-1-N-methyl-3-benzylidene-6-(2R-methyl-3-hydroxypropylidene)piperazine-2,5-dione (2), (3Z,6Z)-3- (4-hydroxybenzylidene)-6-isobutylidenepiperazine-2,5-dione (3), (3Z,6Z)-3-((1H-imidazol-5-yl)-methylene)-6-isobutylidenepiperazine-2,5-dione (4), and (3Z,6S)-3-b...

In the title compound, C(24)H(25)N(3)O(4), the pyrrolidine ring adopts an envelope conformation while the pyrrolidine-2'',5''-dione ring adopts a twist conformation. The indoline unit is planar [maximum deviation of -0.050 (9) Å] and forms a dihedral angle of 40.36 (4)° with the methoxy-phenyl ring. Intra-molecular C-H⋯O hydrogen bonds are observed. In the crystal, mol-ecules are linked into a ...

Linear and nonlinear properties of isoindoline-1,3-dione-fullerene-isoindoline-1,3-dione with the five phases were studied. The geometries combination attained using density functional theory DFT/B3LYP/6-31G+(d,p). calculated are static polarizability, anisotropy polarizability first hyperpolarizability at equilibrium geometry. In this article, theoretical design NLO molecules is discussed. res...