mycobacterium smegmatis ptcc 1307 (cip 73.26) was used as a microbial agent to produce androsta-1,4-diene-3,17-dione (add) and androst-4-ene-3,17-dione, two useful precursors in the synthesis of steroid drugs. the side chain of cholesterol, as the substrate, was selectively cleaved in the presence of five enzyme inhibitors. an intermediate structure with intact side chain, cholest-4-ene-3-one, ...

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...

dione); 1 1flOH-P (1 1/?-hydroxyprogesterone; 1 1 /?-hydroxypregn-4ene-3,20-dione); 1 I-0x0-P (1 1-oxoprogesterone; pregn-4-ene-3,11,20trione); 21-d-F (2 I-deoxycortisol; 11/?,17a-dihydroxypregn-4-ene-3,20dione); 2 1 -d-E (2 1-deoxycortisone; 17a-hydroxypregn-4-ene-3,11,20trione); 1 1-deoxycortisol (Reichstein’s substance S ; cortexolone; 1 7 ~ 2 l-dihydroxypregn-4-ene-3,20-dione); DHS (dihydro...

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...

Six new compounds, trans-3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]pyrrolidine-2,5-dione (1), trans-1-hydroxy-3-(4-hydroxyphenyl)-4-isobutylpyrrolidine-2,5-dione (2), cis-3-(4-hydroxyphenyl)-4-isobutyldihydrofuran-2,5-dione (3), 3-(4-hydroxyphenyl)-4-isobutyl-1H-pyrrole-2,5-dione (4), 3-(4-hydroxyphenyl)-4-isobutylfuran-2,5-dione (5), and dimethyl 2-(4-hydroxyphenyl)-3-isobutylmaleate (6), ...