Two new compounds, osmjapterpenoid A () and osmunjaponin A (), along with twenty-six known compounds, were isolated from the roots and rhizomes of Thunb. The chemical structures of them were elaborated by extensive spectroscopic means, including 1D, 2D-NMR and HR-ESI-MS. Compound is a diterpenoid derived from cembrane with a novel skeleton of 5/13 dicyclic ring system. The possible biogentic pathway of was deduced. Compounds and exhibited moderate inhibition on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages with IC value of 32.09 and 19.81 μM, respectively.
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http://dx.doi.org/10.1080/14786419.2024.2362427 | DOI Listing |
Inorg Chem
January 2025
Institute of Solid State Physics, TU Wien, A-1040 Vienna, Austria.
A novel ternary boride, NiPtB ( = 0.5), was obtained by argon-arc melting of the elements followed by annealing at 750 °C. It exhibits a new structure type with the space group ( = 2.
View Article and Find Full Text PDFJ Med Chem
January 2025
Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.
Despite recent advances in the inhibition of EGFR (epidermal growth factor receptor), there remains a clinical need for new EGFR Exon20 insertion (Ex20Ins) inhibitors that spare EGFR WT. Herein, we report the discovery and optimization of two chemical series leading to ether and biaryl as potent, selective, and brain-penetrant inhibitors of Ex20Ins mutants. Building on our earlier discovery of alkyne which allowed access to CNS property space for an Ex20Ins inhibitor, we utilized structure-based design to move to lower lipophilicity and lower CL compounds while maintaining a WT selectivity margin.
View Article and Find Full Text PDFEnviron Toxicol Chem
January 2025
Oak Ridge Associated Universities (ORAU), Duluth, MN, United States.
Although banned long ago in many countries and jurisdictions, the organochlorine pesticide dichlorodiphenyltrichloroethane (DDT) and compounds related to it remain in the aquatic environment, particularly in sediments, and can pose risks to aquatic life. To inform ecological risk assessment of these compounds, we tested the toxicity of six DDT congeners, specifically the p, p' (4,4') forms of DDT, dichlorodiphenyldichloroethylene (DDE), dichlorodiphenyldichloroethane (DDD), and dichlorodiphenylchloroethylene (DDMU), as well as the o, p' (2,4') isomers of DDT and DDD. The epibenthic amphipod, Hyalella azteca, was exposed for 7 days to waterborne chemical and assessed for changes in survival and growth.
View Article and Find Full Text PDFPLoS One
January 2025
Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
This study presents T-1-NBAB, a new compound derived from the natural xanthine alkaloid theobromine, aimed at inhibiting VEGFR-2, a crucial protein in angiogenesis. T-1-NBAB's potential to interacts with and inhibit the VEGFR-2 was indicated using in silico techniques like molecular docking, MD simulations, MM-GBSA, PLIP, essential dynamics, and bi-dimensional projection experiments. DFT experiments was utilized also to study the structural and electrostatic properties of T-1-NBAB.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Ritsumeikan University: Ritsumeikan Daigaku, Applied Chemistry, B805 Biolink, 1-1-1 Nojihigashi, 525-8577, Kusatsu, JAPAN.
Inorganic photochromic materials offer several advantages over organic compounds, including relatively inexpensive and higher thermal stability. However, tuning their color with the same component has remained a significant challenge. In this study, we demonstrate that the photochromic color of Cu-doped ZnS nanocrystals (NCs), which is initially pale yellow before light irradiation, can be tuned from gray to brown by adjusting the surface stoichiometry of Zn and S, which is controlled through the use of thiol and non-thiol ligands.
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