21370-57-0Relevant articles and documents
Heck Reaction over Pd-Loaded ETS-10 Molecular Sieve
Waghmode, Suresh Babasaheb,Wagholikar, Smita Girish,Sivasanker, Subramanian
, p. 1989 - 1992 (2003)
ETS-10 molecular sieve has been used as a catalyst in the shape-selective photo catalytic decomposition of aromatic molecules, Aldol-type condensations, aniline oxidation, acylation reactions, and alcohol dehydrogenation. The carbon-carbon coupling of different aryl halides with ethyl acrylate over Pd-loaded ETS-10 was presented. The influences of the Pd content, nature of the base and reactivity of the different substrates and reactants on the coupling reaction were presented. The catalyst exhibited high activity and selectivity towards the carbon-carbon coupling of aryl halides with olefins, even at low concentrations of palladium (0.009 to 1.4 mole % with respect to the substrate). In the case of the coupling of ethyl acrylate with iodobenzene, 96% conversion of iodobenzene with > 98% selectivity could be obtained within 1 hr over a 0.2 wt % Pd-loaded catalyst. The catalyst activated aryl bromide and chloride substrates, and was heterogeneous. Aryl bromide, chloride and their derivatives exhibited moderate activity with ethyl acrylates. Organic bases led to higher catalytic activity than inorganic bases. The catalysts could be reused and reactivated by washing with a moderate decrease in activity. The substrate reactivity increased with electron-withdrawing substituents.
Discovery of a novel inhibitor of nitric oxide production with potential therapeutic effect on acute inflammation
Zhu, Long-Qing,Fan, Xiao-Hong,Li, Jun-Fang,Chen, Jin-Hong,Liang, Yan,Hu, Xiao-Ling,Ma, Shu-Meng,Hao, Xiang-Yong,Shi, Tao,Wang, Zhen
supporting information, (2021/05/26)
Inflammation as a host's excessive immune response to stimulation, is involved in the development of numerous diseases. To discover novel anti-inflammatory agents and based on our previous synthetic work on marine natural product Chrysamide B, it and a series of derivatives were synthesized and evaluated for their anti-inflammatory activity on inhibition of LPS-induced NO production. Then the preliminary structure–activity relationships were conducted. Among them, Chrysamide B is the most potent anti-inflammatory agent with low cytotoxicity and strong inhibition on the production of NO (IC50 = 0.010 μM) and the activity of iNOS (IC50 = 0.082 μM) in LPS-stimulated RAW 264.7 cells. Primary studies suggested that the mechanism of action may be that it interfered the formation of active dimeric iNOS but not affected transcription and translation. Furthermore, its good performance of anti-inflammatory effect on LPS-induced multiple inflammatory cytokines production, carrageenan-induced paw edema, and endotoxin-induced septic mice, was observed. We believe that these findings would provide an idea for the further modification and research of these analogs in the future.
Copper-Photocatalyzed Contra-Thermodynamic Isomerization of Polarized Alkenes
Bouillon, Jean-Philippe,Brégent, Thibaud,Poisson, Thomas
supporting information, p. 7688 - 7693 (2020/10/09)
The contra-thermodynamic isomerization of α- and β-substituted cinnamate derivatives catalyzed by the Cu(OAc)2/rac-BINAP complex under blue light irradiation is reported. The use of an oxazolidinone template, which favored the complexation of the copper catalyst to the substrate, allowed the E → Z isomerization of the catalytically formed chromophore under simple and robust reaction conditions in good to excellent ratios. The mechanism of this process based on the transient formation of a chromophore was also studied.
Synthesis and discovery of 18β-glycyrrhetinic acid derivatives inhibiting cancer stem cell properties in ovarian cancer cells
Li, Xiaojing,Liu, Yihua,Wang, Na,Liu, Yuyu,Wang, Shuai,Wang, Hongmin,Li, Aihua,Ren, Shaoda
, p. 27294 - 27304 (2019/09/12)
Despite advances in ovarian cancer treatment, the five-year overall survival rate is less than 30% with the presence of cancer stem cells (CSCs). To develop CSC-targeting therapy, a series of 18β-glycyrrhetinic acid (GA) derivatives containing cinnamamide moiety have been designed, synthesized, and screened for their antiproliferative activity in SKOV3 and OVCAR3 cells. Most of the compounds exhibited stronger antiproliferative activity than GA, and compound 7c was the most active one. Further biological studies showed that compound 7c could induce apoptosis and suppress migration. In addition, compound 7c could not only observably decrease the colony formation and sphere formation ability, but also significantly reduce the CD44+, CD133+, and ALDH+ subpopulation in SKOV3 and OVCAR3 cells. In conclusion, these results indicate that compound 7c is a promising anti-CSC agent for further anti-ovarian cancer studies.
