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Modeling, synthesis and cell-based evaluation of pyridine-substituted analogs of CD3254 and fluorinated analogs of CBt-PMN as novel therapeutics.
Bioorg Med Chem
January 2025
School of Mathematical and Natural Sciences, New College of Interdisciplinary Arts and Sciences, Arizona State University, 4701 W. Thunderbird Road, Glendale, AZ 85308, USA. Electronic address:
Six pyridine analogs of (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid-or CD3254 (11)-in addition to two novel analogs of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-benzo[d][1,2,3]triazole-5-carboxylic acid (CBt-PMN or 23) were prepared and evaluated for selective retinoid-X-receptor (RXR) agonism alongside bexarotene (1), an FDA-approved drug for cutaneous T-cell lymphoma (CTCL). Treatment with 1 often elicits side-effects by disrupting or provoking other RXR-dependent nuclear receptors and cellular pathways. All analogs were assessed through modeling for their ability to bind RXR and then evaluated in human colon and kidney cells employing an RXR-RXR mammalian-2-hybrid (M2H) system and in an RXRE-controlled transcriptional assay.
View Article and Find Full Text PDFNontarget Analysis and Characterization of a Group of Abundant Polyfluoroalkyl Substances─Fluorinated Benzoylurea Pesticides and Their Analogues and Transformation Products in Fish by LC-HRMS and Chemical Species-Specific Algorithms.
J Agric Food Chem
January 2025
Guangdong Key Laboratory of Environmental Resources Utilization and Protection, State Key Laboratory of Organic Geochemistry, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Guangzhou 510640, China.
Poly- and perfluoroalkyl substances (PFASs) are a large class of fluorinated chemicals used in various industrial and agrochemical products such as fluorinated benzoylurea (FBU) pesticides. Initiated from an incidental and preliminary finding of three high-abundance FBUs in fish, this study implemented nontarget analysis and characterization for FBUs together with their analogues and transformation products (TPs) in fish using liquid chromatography, high-resolution mass spectrometry, and chemical species-specific algorithms. A total of 23 FBU-relevant compounds were found and tentatively/accurately elucidated with structures, including 18 PFASs and 5 non-PFAS compounds, of which 4 were original FBUs, 8 were FBU analogues, and 11 were FBU-TPs.
View Article and Find Full Text PDFThe Rise and Risks of Fluorinated Pesticides: A Call for Comprehensive Research to Address Environmental and Health Concerns.
J Agric Food Chem
January 2025
Lautenberg Environmental Health Sciences Laboratory, Department of Environmental Medicine and Climate Science, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
A Fluorine-Functionalized Tb(III)-Organic Framework for Ba Detection.
Molecules
December 2024
School of Food and Pharmaceutical Engineering, Zhaoqing University, Zhaoqing 526061, China.
The development of lanthanide-organic frameworks (Ln-MOFs) using for luminescence sensing and selective gas adsorption applications is of great significance from an energy and environmental perspective. This study reports the solvothermal synthesis of a fluorine-functionalized 3D microporous Tb-MOF with a face-centered cubic () topology constructed from hexanuclear clusters (TbO) bridged by fdpdc ligands, formulated as {[Tb(fdpdc)(-OH)(HO)]·4DMF} (), (fdpdc = 3-fluorobiphenyl-4,4'-dicarboxylate). Complex displays a 3D framework with the channel of 7.
View Article and Find Full Text PDFThe potential endocrine-disrupting of fluorinated pesticides and molecular mechanism of EDPs in cell models.
Ecotoxicol Environ Saf
January 2025
State Key Lab, Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences/Key Laboratory of Agro-products Quality and Safety Control in Storage and Transport Process/Laboratory of Agro-products Quality Safety Risk Assessment, Ministry of Agriculture and Rural Affairs, Beijing 100193, PR China. Electronic address:
Environmental endocrine disruptors constitute a category of exogenous compounds that interfere with the endocrine system's functions in organisms or cells. As a class of particularly representative endocrine-disrupting chemicals, the accumulation of per- and polyfluoroalkyl substances potentially leads to adverse health effects, including hormonal disruptions, developmental issues, and cancer. However, the classification of these disruptors is intricate, and the data on their potential health risks is scattered.
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