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This article discusses the design and synthesis of heterocyclic core scaffolds for drug discovery research. The researchers were able to generate unique heterocyclic skeletons from a common derivative and discovered that an amino moiety could be added to the ring system through annulative reactions with quinones. The target compound possesses both carbonyl and amino groups, similar to biologically active quinones. The researchers optimized the reaction conditions and found that the use of Cu(OAc)2 as a catalyst provided the desired product in high yield. The synthesis of various compounds was also explored. These compounds were tested for their anticancer effects and showed good inhibitory activities against human hepatocellular cells and prostate adenocarcinoma cells. The study suggests that these compounds could be further developed as potential anticancer agents for the treatment of liver and prostate cancer. The given text provides data and information related to the synthesis and characterization of compounds 4a, 4b, 4c, 4d, and 4e. The compounds were synthesized using a general procedure involving the reaction of naphthoquinone with different reagents. The compounds were obtained in good yields and characterized using various techniques such as NMR and HRMS. The data presented in the text can be used by researchers studying the cytotoxic effects of these compounds on HepG2 and PC-3 cells. The document provides information on the synthesis and characterization of various compounds. The compounds are described in terms of their chemical structures [Extracted from the article]

The epidermal growth factor receptor (EGFR), also known as ErbB1 and HER1, belongs to the receptor tyrosine kinase family. EGFR serves as the primary driver in non-small-cell lung cancer (NSCLC) and is a promising therapeutic target for NSCLC. In this study, we synthesized a novel chemical library based on a benzofuran–indole hybrid scaffold and identified 8aa as a potent and selective EGFR inhibitor. Interestingly, 8aa not only showed selective anticancer effects against NSCLC cell lines, PC9, and A549, but it also showed significant inhibitory effects against the double mutant L858R/T790M EGFR, which frequently occurs in NSCLC. In addition, in PC9 and A549 cells, 8aa potently blocked the EGFR signaling pathway, cell viability, and cell migration. These findings suggest that 8aa, a benzofuran–indole hybrid derivative, is a novel EGFR inhibitor that may be a potential candidate for the treatment of NSCLC patients with EGFR mutations. [ABSTRACT FROM AUTHOR]

ABSTRACT Osteopenic diseases, such as osteoporosis, are characterized by progressive and excessive bone resorption mediated by enhanced receptor activator of nuclear factor-κB ligand (RANKL) signaling. Therefore, downregulation of RANKL downstream [...]

Our objective in this study was to determine whether a mitochondda-targeted vitamin E derivative (MitoVit E) would decrease oxidative stress and associated obesity by preventing a previously proposed aconitase inhibition cascade. Sixty-four mice were fed a high-fat (HF) diet for 5 wk. They were then switched to either a low-fat (LF) or a medium-fat (MF) diet and gavaged with MitoVit E (40 mg MitoVit E kg body [weight.sup.-1]) or drug vehicle (10% ethanol in 0.9% NaCl solution) every other day for 5 wk. Epididymal fat weight, as well as liver lipid and remaining carcass lipid, were significantly lower in the MF group receiving MitoVit E (MF-E) than in the MF group receiving vehicle only (MF-C). Liver mitochondrial [H.sub.2][O.sub.2] production and the protein carbonyl level were also significantly lower in MF-E than in MF-C mice. In contrast, none of the biochemical variables (aconitase activity, ATP and [H.sub.2][O.sub.2] production, and protein carbonyl level) in the muscle mitochondria were modified by MitoVit E in either MF or LF groups. Expression of acetyl-CoA carboxylase and fatty acid synthase in both liver and adipose tissue of MF groups was not affected by MitoVit E. However, expression of carnitine palmitoyltransferase 1 a in the liver and uncoupling protein 2 in adipose tissue were significantly enhanced by MitoVit E in both LF and MF groups. In conclusion, MitoVit E attenuates hepatic oxidative stress and inhibits fat deposition in mice but not through alleviation of the aconitase inhibition cascade. doi: 10.3945/jn.110.121715.