Synthesis of Phenolic Coumestans via a Sequential Dehydrogenation/Oxa-Michael Addition Reaction of 2',4'-Dihydroxyl-3-arylcoumarins.

A facile and practical approach for the synthesis of natural coumestans and derivatives starting from 2',4'-dihydroxyl-3-arylcoumarins has been developed. The process involved a seqential intramolecular dehydrogenation/oxa-Micheal reaction efficiently promoted by 1,8-diazabicyclo[5.4.0]undec-7-ene at 40 °C under metal- and ligand-free conditions with good functional group compatibility.

Design, synthesis, and physicochemical study of a biomass-derived CO2 sorbent 2,5-furan-bis(iminoguanidine).

In this study, the concept of biomass-based direct air capture is proposed, and the aminoguanidine CO2 chemical sorbent 2,5-furan-bis(iminoguanidine) (FuBIG) was designed, synthesized, and elucidated for the physicochemical properties in the process of CO2 capture and release. Results showed that the aqueous solution of FuBIG could readily capture CO2 from ambient air and provided an insoluble tetrahydrated carbonate salt FuBIGH2(CO3) (H2O)4 with a second order kinetics. Hydrogen binding modes of iminoguanidine cations with carbonate ions and water were identified by single-crystal X-ray diffraction analysis. Equilibrium constant (K) and the enthalpies (ΔH) for CO2 absorption/release were obtained by thermodynamic and kinetic analysis (K7 = 5.97 × 104, ΔH7 = -116.1 kJ/mol, ΔH8 = 209.31 kJ/mol), and the CO2-release process was conformed to the geometrical phase-boundary model (1-(1-α)1/3 = kt). It was found that the FuBIGH2(CO3) (H2O)4 can release CO2 spontaneously in DMSO without heating. Zebrafish models revealed a favorable biocompatibility of FuBIG.

Copper-Catalyzed Lactamization of (E)-2-(2-Bromophenyl)-3-arylacrylamides for the Synthesis of (E)-3-Arylideneindolin-2-ones.

A copper-catalyzed, ligand-free intramolecular C-N coupling of (E)-2-(2-bromophenyl)-3-arylacrylamides has been developed. This protocol provides an efficient and practical synthetic route for the biologically important (E)-3-arylideneindolin-2-ones from o-bromophenylacetic acids and aromatic or conjugated alkenyl aldehydes. Readily available starting materials, mild and noble metal-free conditions, high efficiency, and good tolerability for phenolic hydroxyl groups make this approach attractive and applicable.

Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFRL858R/T790M inhibitors.

Lung cancer is the leading cause of cancer deaths. It has been demonstrated that epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) are efficacious in patients with EGFR mutation-positive non-small cell lung cancer (NSCLC). In this work, a new series of 2,4-diaryl pyrimidine derivatives containing cyclopropyl moiety were designed, synthesized and evaluated as novel selective EGFRL858R/T790M inhibitors. The most promising compound, 8l demonstrated excellent kinase inhibitory activity against EGFR double mutation with IC50 value of 0.26 nM. Moreover, 8l provided strong activity against H1975 cells with IC50 value of 0.008 µM and exhibited little toxicity toward four non-tumorigenic cell lines. Furthermore, 8l showed potent anti-tumor efficacy in a murine EGFRL858R/T790M-driven H1975 xenograft model. These results indicated that 8l may be a promising drug candidate for further study.

Spatial Distribution, Sources Apportionment and Health Risk of Metals in Topsoil in Beijing, China.

In order to acquire the pollution feature and regularities of distribution of metals in the topsoil within the sixth ring road in Beijing, a total of 46 soil samples were collected, and the concentrations of twelve elements (Nickel, Ni, Lithium, Li, Vanadium, V, Cobalt, Co, Barium, Ba, Strontium, Sr, Chrome, Cr, Molybdenum, Mo, Copper, Cu, Cadmium, Cd, Zinc, Zn, Lead, Pb) were analyzed. Geostatistics and multivariate statistics were conducted to identify spatial distribution characteristics and sources. In addition, the health risk of the analyzed heavy metals to humans (adult) was evaluated by an U.S. Environmental Protection Agency health risk assessment model. The results indicate that these metals have notable variation in spatial scale. The concentration of Cr was high in the west and low in the east, while that of Mo was high in the north and low in the south. High concentrations of Cu, Cd, Zn, and Pb were found in the central part of the city. The average enrichment degree of Cd is 5.94, reaching the standard of significant enrichment. The accumulation of Cr, Mo, Cu, Cd, Zn, and Pb is influenced by anthropogenic activity, including vehicle exhaustion, coal burning, and industrial processes. Health risk assessment shows that both non-carcinogenic and carcinogenic risks of selected heavy metals are within the safety standard and the rank of the carcinogenic risk of the four heavy metals is Cr > Co > Ni > Cd.