Flavonoids are natural polyphenolic compounds and constitute a major class of plant secondary metabolites. To date, structures of more than 10,000 different flavonoids have been elucidated, and most of them are present in cells and tissues of plant parts. Flavonoids have been reported to exert multiple physiological activities and are also consumed as dietary supplements. Flavonoids have been extensively explored as anticancer, anti-inflammatory, antidiabetic, antirheumatic, antioxidant, antimalarial, neuroprotective, cardioprotective, anti-angiogenic, and antiproliferative agents. Most of the flavonoids are biosynthesized in plants via the phenylpropanoid pathway. However, they are associated with some limitations. Chemical synthesis is an alternative strategy to improve the yield and obtain purified products but is hampered by drawbacks, such as intolerance to stressful lab conditions. Pharmacokinetics is the rate-limiting step defining the bioavailability and metabolism of flavonoids, though greatly influenced by their chemical structure. However, nanoformulation is an emerging technique to improve biopharmaceutical fate and achieve target drug delivery. Thus, much attention should be given to identifying other possible chemical approaches for synthesizing flavonoids and improving their pharmacokinetic profiling, hence potentiating their efficacy in clinic.
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http://dx.doi.org/10.2174/1389557523666230214101821 | DOI Listing |
Angew Chem Int Ed Engl
January 2025
University of California Riverside, Chemistry Department, Chemistry Department, 92521, Riverside, UNITED STATES OF AMERICA.
Although metal-organic frameworks are coordination-driven assemblies, the structural prediction and design using metal-ligand interactions can be unreliable due to other competing interactions. Leveraging non-coordination interactions to develop porous assemblies could enable new materials and applications. Here, we use a multi-module MOF system to explore important and pervasive impact of ligand-ligand interactions on metal-ligand as well as ligand-ligand co-assembly process.
View Article and Find Full Text PDFMol Divers
January 2025
School of Biological & Chemical Engineering, Zhejiang University of Science & Technology, Hangzhou, 310023, People's Republic of China.
The quinazoline scaffold serves as a fundamental framework, demonstrating potent anti-tumor activity. Employing the pharmacophore-based scaffold hopping principle, we successfully synthesized a series of FAK/PLK1 inhibitors incorporating the quinazoline scaffold. The synthesized compounds were characterized using H NMR, C NMR, and HRMS techniques.
View Article and Find Full Text PDFMol Divers
January 2025
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai, People's Republic of China.
Succinate dehydrogenase (SDH) has been identified as one of the ideal targets for the development of novel nematicides. However, the resistance of nematodes to fluopyram, one of the commercialized SDH inhibitors, is becoming a growing concern. Since expanding the structural diversity around an active scaffold is a useful strategy for drug development, herein a series of fluopyram analogues with a broad, biologically relevant indole moiety were synthesized and evaluated for nematicidal activity against C.
View Article and Find Full Text PDFBiodegradation
January 2025
Department of Biology, Faculty of Mathematics and Natural Sciences, Universitas Negeri Jakarta, Rawamangun, Jakarta Timur, Indonesia.
Per- and polyfluoroalkyl substances (PFAS) are synthetic organofluoride compounds, widely used in industries since the 1950s for their hydrophobic properties. PFAS contamination of soil and water poses significant environmental and public health risks due to their persistence, chemical stability, and resistance to degradation. The Chemical Abstracts Service catalogs approximately 4300 PFAS globally.
View Article and Find Full Text PDFArch Microbiol
January 2025
Department of Chemistryand Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University Júlio de Mesquita Filho, São José do Rio Preto, SP, Brazil.
Candida is a commensal fungus of clinical interest that commonly lives in oral cavity and intestine but can become an opportunist microrganism and cause severe infections. A serie of 10 aminochalcones were designed and synthetized to obtain compounds anti-Candida with potent and broad-spectrum activity. The most active compound J34 demonstrated excellent in vitro activity against Candida albicans, Candida tropicalis, Candida parapsilosis, Candida glabrata and Candida krusei with minimum inhibitory concentration between 1.
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