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Described here is the R3P/ICH2CH2I-promoted dehydroxylative sulfonylation of alcohols with a variety of sulfinates. In contrast to previous dehydroxylative sulfonylation methods, which are usually limited to active alcohols, such as benzyl, allyl, and propargyl alcohols, our protocol can be extended to both active and inactive alcohols (alkyl alcohols). Various sulfonyl groups can be incorporated, such as CF3SO2 and HCF2SO2, which are fluorinated groups of interest in pharmaceutical chemistry and the installation of which has received increasing attention. Notably, all reagents are cheap and widely available, and moderate to high yields were obtained within 15 min of reaction time.
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Digitalisation and technological developments are profoundly changing the socioeconomic structure of society and people's lifestyles, which may have a significant impact on the distribution of income among different groups of people. This study conducted a quantitative investigation into the impact of the digital economy on income inequality based on the skill bias theory. First, empirical model analysis showed that digital economy has a linear dampening effect on income inequality and that there is no non-linear relationship. Then, the study analyzed the mechanisms underlying this relationship, which revealed that mining and remittances suppress income inequality in the presence of digital economy, while government spending promotes income inequality. Finally, heterogeneity analysis indicated that the suppressive impact of digital economy on income inequality in capitalist countries is stronger than in ex-communist countries. These findings will not only help to achieve social equity, but also provide a strategic direction for economic development to make the dividends of the digital economy more inclusive.
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Resveratrol is one of the most interesting naturally-occurring nonflavonoid phenolic compounds with various biological activities, such as anticancer, neuroprotection, antibacterial, and anti-inflammatory. However, there is no clinical usage of resveratrol due to either its poor activity or poor pharmacokinetic properties. Heteroarenes-modified resveratrol is one pathway to improve its biological activities and bioavailability, and form more modification sites. In this review, we present the progress of heteroaryl analogues of resveratrol with promising biological activities in the latest five years, ranging from the synthesis to the structure-activity relationship and mechanism of actions. Finally, introducing heteroarenes into resveratrol is an effective strategy, which focuses on the selectivity of structure-activity relationship in vivo.
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BACKGROUND: Genistein has been limited in clinical application due to its low bioavailability, extremely poor liposolubility, and fast glycosylation rate, though it possesses anti-breast cancer activity. Therefore, the discovery of novel genistein derivatives is an urgency. OBJECTIVE: To enhance the anti-breast cancer activity of genistein, a series of novel fluorinated genistein derivatives were synthesized. METHODS: Their in vitro antitumor activity was investigated by the MTT assay against three cancer cell lines, via, MDA-MB-231, MCF-7, and MDA-MB-435, respectively. RESULTS: Analogs 1d, 2b, and 3b showed remarkable anticancer activities compared to tamoxifen, a clinical anti-breast cancer drug on the market. CONCLUSION: The activities against breast cancer of genistein were enhanced by introducing the 7- alkoxyl group and fluorine atom into the B-ring. Therefore, these compounds may be potential candidates for treating breast cancer.
Assuntos
Antineoplásicos , Neoplasias da Mama , Humanos , Feminino , Genisteína/farmacologia , Genisteína/uso terapêutico , Neoplasias da Mama/patologia , Tamoxifeno/farmacologia , Tamoxifeno/uso terapêutico , Linhagem Celular , Proliferação de Células , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura MolecularRESUMO
P-stereogenic pincer-metal complexes are one of the most interesting pincer type organometallic compounds. Many kinds of this type of complexes were synthesized and used as catalysts in asymmetric catalysis. On the basis of our work in this field, this paper reports the recent progress in P-stereogenic pincer chemistry, including the synthesis of P-stereogenic pincer ligands, the synthesis of P-stereogenic pincer-metal complexes, and the achievements in P-stereogenic pincer-metal complex catalyzed asymmetric synthesis.