In the present study, a new series of -Aminophosphonates bearing 6-amino-1,3-dimethyluracil was synthesized in good to excellent yields (78-95%) by one-pot, three-component reaction of 6-amino-1,3-dimethyluracil, aromatic aldehydes and diethylphosphite Kabachnik-Fields reaction by using an eco-friendly Eaton's reagent. All the compounds were screened for antioxidant studies by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide (HO) methods. Among the synthesized bioactive molecules, , , , and exhibited promising antioxidant activity compared with the standard drug Ascorbic acid. Furthermore, in order to support the biological results of the compounds, molecular docking studies were performed against Aromatase enzyme for four compounds which revealed that the compounds , , , and have significant binding modes, with docking scores of -8.6, -8.4, -8.1 and -8.1 respectively and the compound specifically has equal dock score of -8.0 when compared with the standard drug Exemestane.
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http://dx.doi.org/10.1080/10799893.2020.1722166 | DOI Listing |
Mol Divers
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, 560107, Karnataka, India.
Discoidin domain receptors (DDR) are categorized under tyrosine kinase receptors (RTKs) and play a crucial role in various etiological conditions such as cancer, fibrosis, atherosclerosis, osteoarthritis, and inflammatory diseases. The structural domain rearrangement of DDR1 and DDR2 involved six domains of interest namely N-terminal DS, DS-like, intracellular juxtamembrane, transmembrane juxtamembrane, extracellular juxtamembrane intracellular kinase domain, and the tail portion contains small C-tail linkage. DDR has not been explored to a wide extent to be declared as a prime target for any particular pathological condition.
View Article and Find Full Text PDFAdv Biotechnol (Singap)
January 2025
Singapore Institute of Food and Biotechnology Innovation (SIFBI), Agency for Science, Technology and Research (A*STAR), Singapore, Republic of Singapore.
Enzymes are the cornerstone of biocatalysis, biosynthesis and synthetic biology. However, their applicability is often limited by low substrate selectivity. A prime example is the bifunctional linalool/nerolidol synthase (LNS) that can use both geranyl diphosphate (GPP) and farnesyl diphosphate (FPP) to produce linalool and nerolidol, respectively.
View Article and Find Full Text PDFNat Prod Res
January 2025
Laboratory of Natural Products and Heterocyclic Synthesis, Department of Organic Chemistry, Faculty of Sciences, The University of Yaoundé 1, Yaoundé, Cameroon.
From the leaves of , fourteen compounds were isolated and identified: D-mannitol (), a mixture of β-sitosterol () and stigmasterol (), α-amyrin (), betulin (), lupeol (), lupenone (), betulinic acid (), taraxerol (), 3β-(E)-coumaroyltaraxerol (), 3β-(Z)-coumaroyltaraxerol (), ursolic acid (), stigmasterol 3-O-β-D-glucoside (), and β-sitosterol 3-O-β-D-glucoside (). These compounds were analysed through NMR spectroscopy (both 1D and 2D) and by comparing them to previously published data. Compounds , , , and - have been identified from this species for the first time.
View Article and Find Full Text PDFFuture Med Chem
January 2025
Department of Chemistry, University of Malakand, Dir Lower, Khyber Pakhtunkhwa, Pakistan.
Background: Due to the divers biological applications of Cu(II) complexes, we in this study reports the various Cu(II) complexes. The study aims to synthesize and assess new Cu(II) complexes as powerful β-glucuronidase inhibitors.
Methods: Five Schiff base ligands and their complexes were synthesized, characterized, and screened against β-glucuronidase inhibitory activity.
Heliyon
January 2025
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, 56212, Republic of Korea.
The suppression of tyrosinase (TYR), a key enzyme in melanogenesis, has been suggested as an effective strategy for preventing melanin accumulation. We previously discovered the novel chrysin derivative hydroxyethyl chrysin (HE-chrysin) through an irradiation technique, which exerted higher anti-inflammatory and anti-cancer activities than original chrysin. In the present study, we explored whether HE-chrysin has antioxidant and anti-melanogenic capacity using B16F10 murine melanoma cells and molecular docking.
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