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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 |
Med Sci (Paris)
September 2025
Service des maladies de l'appareil digestif. Centre de compétence Maladies rares « Maladies inflammatoires des voies biliaires et hépatites autoimmunes », Hôpital Huriez, Lille, France.
Primary biliary cholangitis (PBC) is a rare disease for which management long consisted of a single treatment: ursodeoxycholic acid. In 2015-2016, this disease regained interest with the first studies on obeticholic acid (FXR agonist) and then on bezafibrate (PPAR agonist). Subsequently, over the past five years, significant progress has been made in the management of PBC.
View Article and Find Full Text PDFDrug Des Devel Ther
September 2025
Department of Anesthesiology, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, People's Republic of China.
Purpose: This study aimed to compare the analgesic efficacy of liposomal bupivacaine with that of traditional ropivacaine in adductor canal blocks for patients undergoing knee arthroplasty.
Patients And Methods: A total of 119 consenting participants, who were scheduled for elective knee arthroplasty (including total knee replacement and unicompartmental knee replacement) under general anesthesia, were randomly assigned to either receive an ultrasound-guided adductor canal block with ropivacaine or liposomal bupivacaine. The primary endpoint of this study was the pain scores at 2, 24, 48, and 72 hours post-surgery.
Front Endocrinol (Lausanne)
September 2025
de Duve Institute, Faculté de Pharmacie et des Sciences Biomédicales, Université Catholique de Louvain, Brussels, Belgium.
The understanding of the conformational events occurring through the Insulin-like Receptors (ILRs) upon binding of their cognate hormones is very advanced, thanks to multidisciplinary efforts and breakthroughs, from molecular/cell biology to structural studies. However, the full length structures of this class of Tyrosine Kinase (TK) receptors are still not available. This is due to fundamental methodological constraints: a need for lipid micelles or nanodiscs required for the stabilisation of the full-length single receptor molecule.
View Article and Find Full Text PDFOrg Lett
September 2025
Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
An designed benzodioxin fused analogue of a des-(1-hydroxyethyl)-lincomycin analogue was synthesized in a asymmetric fashion from an achiral acylfuran, a 4-(-Pr)--methyl-proline, and catechol. The synthesis of the 6-amino-galactose portion of the lincomycin analogue necessitated the development of a novel stereospecific tandem Pd-glycosylation/1,4-addition reaction between catechol and an -Cbz-protected 6-amino-pyranone with a Pd-π-allyl leaving group at the -1 position. The desired -stereochemistry was installed by a subsequent stereoselective ketone reduction, alcohol elimination, and diastereoselective dihydroxylation of the -3/4 alkene.
View Article and Find Full Text PDFEur J Clin Nutr
September 2025
Centre Régional de Pharmacovigilance, Service de Pharmacologie périnatale, pédiatrique et adulte, Hopital Cochin, Assistance Publique-Hopitaux de Paris (AP-HP), Paris, France.
Although GLP-1 receptors analogues (RAs) benefits-risks profile has been largely documented in diabetes, higher dosages recently approved in obesity still require further assessment. We describe here the case of a 49-year-old female patient treated with semaglutide for obesity, who presented with Wernicke encephalopathy in a context of iterative vomiting and reduced food intake. Eighteen other cases of Wernicke encephalopathy were reported in literature and in the WHO global safety database (VigiBase).
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