Angular pyrrolocoumarins were synthesized from the reaction of 4-hydroxyindole or 5-hydroxyindole with DMAD and PPh(3) and were tested for anti-inflammatory and antioxidant activity. These compounds significantly inhibited the carrageenin-induced paw edema (60.5%-73.4%) and have important scavenging activity. Although their interaction with the free stable radical DPPH is not high, compound 9 is the most potent (73.4%) in the in vivo experiment. Compound 7 seems to be a potent LOX inhibitor. An attempt was made to correlate the biological results with their structural characteristics and physicochemical parameters.
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http://dx.doi.org/10.1080/14756360701400801 | DOI Listing |
Heliyon
November 2024
Institute of Cell Biology and Biophysics, Department of Cell Biology, Leibniz University Hannover, 30419, Hannover, Germany.
Fungal specialized metabolites are known for their potent biological activities, among which tropolone sesquiterpenoids (TS) stand out for their diverse bioactivities. Here, we report cytotoxic and proliferation inhibitory effects of the recently discovered TS compounds 4-hydroxyxenovulene B and 4-dihydroxy norpycnidione, and the structurally related 4-hydroxy norxenovulene B and xenovulene B. Inhibition of metabolic activity after TS treatment was observed in Jurkat, PC-3 and FAIK3-5 cells, whereas MDA-MB-231 cells were unresponsive to treatment.
View Article and Find Full Text PDFJ Biomol Struct Dyn
January 2025
Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
Four organotin(IV) carboxylate complexes; (CH)SnL (), CHSnL (), (CH)SnL () and (CH)SnL () are synthesized by the condensation reaction of organotin(IV) chlorides with sodium-4-chloro-2-methylphenoxyacetate (). The FT-IR spectra suggested bridging/chelating bidentate coordination of the ligand to the tin atom. Single-crystal XRD analysis authenticated the FT-IR findings for and .
View Article and Find Full Text PDFBiomed Chromatogr
February 2025
Yangzhou University Medical College, Jiangsu Key Laboratory of Experimental & Translational Non-coding RNA Research, Institute of Translational Medicine, Yangzhou University, Yangzhou, Jiangsu Province, China.
Mobocertinib is a potent selective tyrosine kinase inhibitor approved for the treatment of non-small cell lung cancer with activating EGFR exon 20 insertions. The aim of this study was to develop a procedure for liquid chromatography tandem mass spectrometry (LC-MS/MS) for the determination of mobocertinib and its metabolite desmethyl-mobocertinib in human plasma. The human plasma samples were precipitated with acetonitrile and analyzed using a Waters ACQUITY BEH C column coupled to a triple quadrupole mass spectrometer.
View Article and Find Full Text PDFSci Rep
January 2025
The Second Affiliated Hospital of Zhejiang Chinese Medical University, Hangzhou, People's Republic of China.
Chronic kidney disease (CKD) stands as a formidable global health challenge, often advancing to end-stage renal disease (ESRD) with devastating morbidity and mortality. At the central of this progression lies podocyte injury, a critical determinant of glomerular dysfunction. Compound K (CK), a bioactive metabolite derived from ginsenoside, has emerged as a compelling candidate for nephroprotective therapy.
View Article and Find Full Text PDFNat Commun
January 2025
Department of Chemistry, Columbia University, New York, NY, USA.
Variants of SARS-CoV-2 have continued to emerge across the world and cause hundreds of deaths each week. Due to the limited efficacy of vaccines against SARS-CoV-2 and resistance to current therapies, additional anti-viral therapeutics with pan-coronavirus activity are of high interest. Here, we screen 2.
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