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A growing number of studies have reported that routinely monitored per- and polyfluoroalkyl substances (PFAS) are not sufficient to explain the extractable organic fluorine (EOF) measured in human blood. In this study, we address this gap by screening pooled human serum collected over 3 decades (1986-2015) in Tromsø (Norway) for >5000 PFAS and >300 fluorinated pharmaceuticals. We combined multiple analytical techniques (direct infusion Fourier transform ion cyclotron resonance mass spectrometry, liquid chromatography-Orbitrap-high-resolution mass spectrometry, and total oxidizable precursors assay) in a three-step suspect screening process which aimed at unequivocal suspect identification. This approach uncovered the presence of one PFAS and eight fluorinated pharmaceuticals (including some metabolites) in human serum. While the PFAS suspect only accounted for 2-4% of the EOF, fluorinated pharmaceuticals accounted for 0-63% of the EOF, and their contribution increased in recent years. Although fluorinated pharmaceuticals often contain only 1-3 fluorine atoms, our results indicate that they can contribute significantly to the EOF. Indeed, the contribution from fluorinated pharmaceuticals allowed us to close the organofluorine mass balance in pooled serum from 2015, indicating a good understanding of organofluorine compounds in humans. However, a portion of the EOF in human serum from 1986 and 2007 still remained unexplained.
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http://dx.doi.org/10.1021/acs.est.4c03758 | DOI Listing |
J Med Chem
September 2025
Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California San Diego, La Jolla, California 92093, United States.
Proteasome inhibitors are effective in treating hematologic cancers but have limited utility in brain tumors due to poor blood-brain barrier (BBB) penetration and metabolic instability. In this study, we developed novel macrocyclic peptide epoxyketone inhibitors with improved drug-like properties. Compounds were screened for cytotoxicity against brain cancer cell lines, permeability (PAMPA-BBB and Caco-2), and metabolic stability.
View Article and Find Full Text PDFOrg Lett
September 2025
Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, China.
Halogenated phenazines hold promise as antimicrobial and antibiofilm agents, yet are mainly accessed via chemical synthesis. Herein, we report PezW, a novel single-component flavin-dependent halogenase (FDH) that halogenates phenazine scaffolds, notably enabling enzymatic synthesis of bioactive 2-bromo-1-hydroxyphenazine () and 2,4-bromo-1-hydroxyphenazine (). Structural modeling and mutagenesis revealed key residues critical for substrate binding and catalysis.
View Article and Find Full Text PDFACS Appl Mater Interfaces
September 2025
School of Textile Science and Engineering, Tiangong University, Tianjin 300387, China.
Triboelectric nanogenerators (TENGs) are typically constrained to operate below 200 °C due to the thermionic emission effect and material degradation at high temperatures. Herein, high-temperature-resistant fluorinated polyimide nanofibers (4,4'-(hexafluoroisopropylidene) diphthalic anhydride-4,4'-oxidianiline/2,2″-bis(trifluoromethyl)benzidine, 6FDA-ODA/TFDB) were designed to mitigate the thermionic emission effect through the introduction of trifluoromethyl (-CF) groups. 6FDA-ODA/TFDB nanofibers exhibited a fine fiber structure and a large highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) gap, which enhanced its effective contact area and maintained more localized states for charge transfer.
View Article and Find Full Text PDFOrg Lett
September 2025
School of Pharmacy and Food Engineering, Wuyi University, Jiangmen 529090, P. R. China.
3-Fluoropyrroles are privileged scaffolds in pharmaceutical and agrochemical applications, yet their synthesis remains challenging. Herein, we report a palladium(0)-catalyzed [4+1] cycloaddition/dehydration strategy for the efficient construction of 3-fluoropyrroles from readily available 3,3-difluoropent-4-en-2-ones and primary amines. This transformation proceeds via C-F bond activation to generate a key π-allyl-Pd(II) intermediate, followed by intramolecular addition/dehydration to furnish the heterocyclic core.
View Article and Find Full Text PDFNat Catal
July 2025
Department of Chemistry, The Scripps Research Institute; 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Despite increasing demand for chiral fluorinated organic molecules, enantioselective C-H fluorination remains among the most challenging and sought-after transformations in organic synthesis. Furthermore, utilizing nucleophilic sources of fluorine is especially desirable for F-radiolabelling. To date, methods for enantioselective nucleophilic fluorination of inert C(sp)-H bonds remain unknown.
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