10.1371/journal.pone.0159316
The study employed a novel approach called disulfide-trapping to identify lead compounds targeting LRH-1. From a library of 1280 disulfide-linked compounds, 28 were found to conjugate with high efficiency to a native cysteine residue (Cys346) in the ligand binding domain of LRH-1. Through computational modeling and cellular assays, the lead compound was further developed into ligands PME8 and PME9, which bind to LRH-1 reversibly and increase its activity in cells. These newly identified ligands showed comparable induction of the LRH-1 dependent target gene CYP24A1 in human HepG2 cells to the existing synthetic agonist RJW100, and their activity was specific as siRNA-mediated knockdown of LRH-1 rendered them ineffective. The chemicals used in the process included the disulfide-linked compound library, β-mercaptoethanol (BME) as a reducing agent, and various reagents for ligand synthesis and cellular assays.
10.1007/BF00633163
The research aimed to synthesize new types of biologically active organosilicon compounds, monomers for silicon-containing polymers, and complexones active with respect to transition metal ions. The study focused on the reactions of 1-(triethylsilyl)aziridine (I) with alkanethiols and 2-mercaptoethanol, as well as the reactions of 1-[2-(trialkylsilyl)ethyl]aziridines with 2-mercaptoethanol and mercaptocarboxylic acids. The IR and PMR spectra of the products were analyzed to confirm their structures. The conclusions drawn from the study indicate that the Si-N bond cleavage rather than the opening of the aziridine ring occurs in the reaction with alkanethiols, and the aziridine ring opens in the reactions with 2-mercaptoethanol and mercaptocarboxylic acids, leading to the formation of biologically active organosilicon compounds.
10.1134/S1070428009070100
The study investigates the synthesis and reactions of pyrazole-4-carbaldehydes. The researchers converted 1-, 3-, and 5-alkylpyrazoles, as well as linearly bridged bis-pyrazoles, into the corresponding 4-formyl derivatives using the Vilsmeier–Haak reaction under standard conditions and microwave activation in DMF. They found that 5-chloro-1,3-dialkyl-1H-pyrazoles did not undergo formylation under these conditions. The study also explored the reaction of 1,1′-bridged bis-3,5-dimethyl-1H-pyrazoles with 2-sulfanylethanol in the presence of chloro(trimethyl)silane to produce bridged bis-4-(1,4,6-oxadithiocan-5-yl)-1H-pyrazoles. The compounds synthesized in this study have potential applications in medicinal chemistry due to the significance of pyrazole rings in many modern drugs.
10.1021/jo9012805
The research aims to study the reactivity of RNA radicals, specifically the 5,6-dihydrouridin-6-yl radical, using photochemical methods. The study employs Norrish type I photocleavage of the tert-butyl ketone (2b) to generate the 5,6-dihydrouridin-6-yl radical (1b) and investigates its reactivity under aerobic and anaerobic conditions. Key chemicals used include ?-mercaptoethanol as a trapping agent, benzoyl groups for enhanced detection via HPLC, and various ribonucleoside derivatives as precursors and product standards. The study finds that the radical can be cleanly generated with high mass balances, and its reactivity is similar to but slightly less than that of its 2'-deoxyribonucleoside analogue. The major product formed in the presence of O2 is 5'-benzoyl-6-hydroxy-5,6-dihydrouridine (6), while under anaerobic conditions, dihydrouridine (4) is the primary product. The study concludes that the 5,6-dihydrouridin-6-yl radical is a useful model for studying RNA radical chemistry and its potential role in oxidative RNA damage.
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