The copper(I)-catalyzed regioselective [3 + 2] cyclization of pyridines toward alkenyldiazoacetates leading to functionalized indolizine derivatives is reported. A broad range of pyridine derivatives (including quinoline and isoquinoline) is compatible with this cyclization reaction. The process represents the first successful example of metal-catalyzed cyclization of a π-deficient heterocyclic system with alkenyldiazo compounds.
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Sci Rep
January 2025
Department of Clinical and Molecular Medicine, Norwegian University of Science and Technology, N-7491, Trondheim, Norway.
The cytotoxic mechanisms of thymidylate synthase inhibitors, such as the multitarget antifolate pemetrexed, are not yet fully understood. Emerging evidence indicates that combining pemetrexed with histone deacetylase inhibitors (HDACi) may enhance therapeutic efficacy in non-small cell lung cancer (NSCLC). To explore this further, A549 NSCLC cells were treated with various combinations of pemetrexed and the HDACi MS275 (Entinostat), and subsequently assessed for cell viability, cell cycle changes, and genotoxic markers.
View Article and Find Full Text PDFNat Commun
January 2025
State Key Laboratory of Drug Research & Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
The efficacy of cancer immunotherapy relies on a sufficient amount of functional immune cells. Triple-negative breast cancer lacks enough immune cell infiltration, and adjuvant therapy is necessary to prime anti-tumor immunity. However, the improvement in efficacy is unsatisfactory with concern about inducing systemic immunotoxicity.
View Article and Find Full Text PDFEnviron Res
January 2025
Key Laboratory of Groundwater Resources and Environment (Jilin University), Ministry of Education, College of New Energy and Environment, Jilin University, Changchun 130021, P. R. China; Jilin Provincial Key Laboratory of Water Resources and Water Environment, College of New Energy and Environment, Jilin University, Changchun 130021, P. R. China. Electronic address:
Phenolic compounds are prevalent in domestic and industrial effluents, leading a serious environmental hazard. Paper-based analysis device mediated by nanozymes has shown great potential in portable visual determination of phenolic compounds in the environment. In this work, we used nicotinic acid derivatives such as pyridine-2,3-dicarboxylic acid, 2-methylnicotinic acid and 2-aminonicotinic acid by coordinating copper (II) acetate monohydrate coordination to obtain Cu2-COOHNA, Cu2-CHNA, Cu2-ANA nanozymes with laccase-activity.
View Article and Find Full Text PDFJ Med Chem
January 2025
Xi'an Key Laboratory for Antiviral and Antimicrobial-Resistant Bacteria Therapeutics Research, Xi'an 710021, China.
Multidrug-resistant (MDR) bacteria pose a global health threat, underscoring the need for new antibiotics. Lefamulin, the first novel-mechanism antibiotic approved by the FDA in decades, showcases pleuromutilins' promise due to low mutation frequency. However, their clinical use is limited by poor pharmacokinetics and organ toxicity.
View Article and Find Full Text PDFSci Adv
January 2025
School of Chemistry and Chemical Engineering, Zhangjiang Institute for Advanced Study, Frontiers Science Center for Transformative Molecules, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, Shanghai 200240, P. R. China.
Metal single atoms are of increasing importance in catalytic reactions. However, the mass diffusion is yet substantially limited by the confined surface of the support in comparison to homogeneous catalysis. Here, we demonstrate that cylindrical micellar brushes with highly solvated poly(2-vinylpyridine) coronas can immobilize 33 types of metal single atoms with 8.
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