Desmosdumotin C (Des C), a natural product isolated from the roots of , has shown good antitumor activity. A three dimensional quantitative structure-activity relationship (QSAR) study using the comparative molecular field analysis (CoMFA) method was performed on 32 Des C analogues. Based on the QSAR, 18 new Des C analogues were designed and synthesized. An efficient three-step synthetic strategy toward Des C and its analogues was developed from commercial available 2, 4, 6-trihydroxyacetophenone. All synthesized compounds were evaluated against a panel of human cancer cell lines and showed ED values ranging from 1.1 to 25.1 µΜ.
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http://dx.doi.org/10.1080/10286020.2018.1473383 | DOI Listing |
J Comput Aided Mol Des
December 2024
Amity Institute of Biotechnology, Amity University Uttar Pradesh, Sector-125, Noida, UP, 201313, India.
Diabetes represents a significant global health challenge associated with substantial healthcare costs and therapeutic complexities. Current diabetes therapies often entail adverse effects, necessitating the exploration of novel agents. Glucokinase (GK), a key enzyme in glucose homeostasis, primarily regulates blood glucose levels in hepatocytes and pancreatic cells.
View Article and Find Full Text PDFChemistry
December 2024
Technische Universitat Berlin, Chemistry, Strasse des 17. Juni 135, Sekr. C2, 10623, Berlin, GERMANY.
Water-assisted electrocatalytic oxidation of alcohols into valuable chemicals is a promising strategy to circumvent the sluggish kinetics of water oxidation, while also reducing cell voltage and improving energy efficiency. Recently, transition metal (TM)-based catalysts have been investigated for anodic alcohol oxidation, but success has been limited due to competition from the oxygen evolution reaction (OER) within the working regime. In this study, NiCo-based Prussian blue analog (PBA) was electrochemically activated at the anodic potential to produce a Co-Ni(O)OH active catalyst with a nanosheet-like architecture.
View Article and Find Full Text PDFAliment Pharmacol Ther
December 2024
Sorbonne Université, INSERM, Institut Pierre Louis d'Épidémiologie et de Santé Publique, IPLESP, Paris, France.
Background: Conflicting results have been reported on the impact of tenofovir versus entecavir on liver-related outcomes.
Aims: To explore trends in clinical outcomes in chronic hepatitis B virus (HBV)-infected patients and compare the impact of tenofovir versus entecavir on the risk of hepatocellular carcinoma (HCC), liver transplantation (LT) and mortality.
Methods: We used the French National Health Insurance Databases (SNDS) to identify HBV-infected patients.
Front Immunol
December 2024
Centre National de la Recherche Scientifique (CNRS) Unité Mixte de Recherche (UMR), Université Paris Cité, Paris, France.
Introduction: Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by an overactive immune response, particularly involving excessive production of type I interferons. This overproduction is driven by the phosphorylation of IRF7, a crucial factor in interferon gene activation. Current treatments for SLE are often not very effective and can have serious side effects.
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December 2024
Physiologie de la Reproduction et des Comportements, CNRS, INRAE, Université de Tours, 37380 Nouzilly, France.
Intravaginal sponges impregnated with the progesterone (P4) analogue fluorogestone acetate (FGA) induce synchronous oestrous behaviour and normal ovulatory cycle in goats. To explore alternatives using natural P4 from plants, we developed a method of ethanolic extraction and a specific enzyme immunoassay (EIA) to measure P4 in the different parts of the walnut tree Juglans regia. We found a very high concentration of P4, specifically in the leaves of the three most common French varieties (∼100 mg/kg of DM) but not in flowers, fruits, septa, husk, oil or cake.
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