Using the methodology of "click" chemistry, a series of conjugates of 3,5-bis(benzylidene)-1-(prop-2-yn)piperidin-4-ones with 4-alkyl-3-azidomethyl-2-ethoxy-2,5-dihydro-5H-1,2 oxaphosphol 2-oxides was synthesized. All newly obtained compounds 8-18 were characterized by H, C, P, F NMR and IR spectroscopy. The potential antitumor activity of the synthesized conjugates8-18was studied in terms of their ability to influence the viability of variouscancercell lines, including A549, SH-SY5Y, Hep-2, and HeLa. Compound 15, which contains two fluorine atoms in the benzene ring, was shown to be the most promising. The mechanism of the cytotoxic action of this conjugate is supposed to be associated with the ability to inhibit the glycolytic profile of transformed cells.
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http://dx.doi.org/10.1016/j.bmcl.2022.128940 | DOI Listing |
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFCancer Med
January 2025
Department of Pharmacology, College of Pharmacy, Jinan University, Guangzhou, China.
Background: Distinctive heterogeneity characterizes diffuse large B-cell lymphoma (DLBCL), one of the most frequent types of non-Hodgkin's lymphoma. Mitochondria have been demonstrated to be closely involved in tumorigenesis and progression, particularly in DLBCL.
Objective: The purposes of this study were to identify the prognostic mitochondria-related genes (MRGs) in DLBCL, and to develop a risk model based on MRGs and machine learning algorithms.
J Agric Food Chem
January 2025
College of Ocean Food and Biological Engineering, Jimei University, Xiamen 361021, China.
In this study, we present an intelligent electromagnetic-actuated microfluidic chip integrated with a G-quadruplex DNAzyme-based biocatalysis platform for rapid and sensitive tetracycline (TC) detection. In this sensing system, TC significantly quenches fluorescent magnetic carbon dots (M-CDs) via the internal filtration effect and dynamic quenching (the excitation and emission wavelength at 350 and 440 nm, respectively). Then, the G-quadruplex on the M-CDs-Aptamer is exposed and bound with hemin to form hemin-G-quadruplex DNAzyme, catalyzing the conversion of 3,3',5,5'-tetramethylbenzidine to produce blue color.
View Article and Find Full Text PDFJ Agric Food Chem
January 2025
Tianjin Key Laboratory of Food Science and Health, School of Medicine, Nankai University, Tianjin 300071, China.
This study has developed a pressure sensor array based on four functionalized DNA-nanoenzymes with catalase-like activity for multiple detections of foodborne pathogens through a portable pressure manometer. Benefiting from functionalization of 4-mercaptophenylboronic acid and β-mercaptoethylamine, the diversity of nonspecific interactions between four DNA-nanoenzymes and each of the nine bacteria leads to differences in pressure response patterns by catalyzing HO to generate exclusive "fingerprints". As effective statistical tools for processing multivariate data, principal component analysis and hierarchical clustering analysis are employed to identify nine foodborne pathogens by analyzing pressure response patterns.
View Article and Find Full Text PDFJ Agric Food Chem
January 2025
College of Food Science and Engineering, Northwest A&F University, Yangling, 712100 Shaanxi, China.
Pumpkin extract has been shown to alleviate hyperglycemic symptoms by improving glucose metabolism disorders. However, the specific active components responsible for its hypoglycemic effects and the underlying molecular mechanisms remain unclear. In this study, db/db mice underwent a 4-week dietary intervention with two pumpkin flours (PF1 and PF2), total dietary fiber (TDF), soluble dietary fiber (SDF), and insoluble dietary fiber (IDF), with acarbose serving as a positive control.
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