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Discovery of novel thienopyridine indole derivatives as inhibitors of tubulin polymerization targeting the colchicine-binding site with potent anticancer activities.
Eur J Med Chem
January 2025
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:
Based on the molecular hybridization strategy, novel thienopyridine indole derivatives were designed and synthesized as tubulin polymerization inhibitors, and the in vitro antiproliferative potency on MGC-803, KYSE450 and HCT-116 cells was evaluated. Among them, compound 20b showed a broad-spectrum antiproliferative activity against 11 cancer cell lines, with IC values below 4 nmol/L. Notably, it demonstrated exceptional efficacy against MGC-803 (IC = 1.
View Article and Find Full Text PDFEffectiveness of Anti-Inflammatory Agents to Prevent Atrial Fibrillation After Cardiac Surgery: A Systematic Review and Network Meta-Analysis.
CJC Open
January 2025
Division of Respirology, Department of Medicine, University of Toronto, Toronto, Ontario, Canada.
Background: Preventing postoperative atrial fibrillation (POAF) as one of the most significant complications of cardiovascular surgeries remains a major clinical challenge. We conducted a systematic review with network meta-analysis of randomized controlled trials, to identify the most effective and safe anti-inflammatory drugs to prevent new-onset POAF.
Methods: MEDLINE, Embase, Web of Science, and Cochrane Library were searched without language or publication-date restriction on August 8, 2022 (updated on August 8, 2023).
Role of ivermectin and colchicine in the treatment of COVID-19: a randomized controlled clinical trial.
J Infect Dev Ctries
December 2024
Internal Medicine Department, Faculty of Medicine, Ain Shams University, Cairo, Egypt.
Introduction: The objective of this study was to assess the effectiveness of ivermectin and colchicine as treatment options for coronavirus disease 2019 (COVID-19).
Methodology: A three-arm randomized controlled clinical trial was conducted in the Triage Clinic of the family medicine department at Ain Shams University Hospitals on participants who had been diagnosed with moderate COVID-19. Patients aged < 18 years or > 65 years, with any co-morbidities, pregnant or lactating females, and those with mild or severe COVID-19 confirmed cases were excluded.
The Anthelmintic Activity of Lam. Against Gastrointestinal Nematodes of Sheep: Rosmarinic Acid Quantification and In Silico Tubulin-Binding Studies.
Pathogens
January 2025
Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Ankara 06330, Turkey.
Gastrointestinal nematodes (GINs) inflict significant economic losses on sheep and goat farming globally due to reduced productivity and the development of anthelmintic resistance. Sustainable control strategies are urgently needed including the exploration of medicinal plants as safer alternatives to chemical anthelmintics. This genus of plants is used for anti-inflammatory, antioxidant, and antimicrobial activities.
View Article and Find Full Text PDFSynthesis and Biological Evaluation of New -Restricted Triazole Analogues of Combretastatin A-4.
Molecules
January 2025
Department of Organic Chemistry, University of Valencia, E-46100 Burjassot, Spain.
The natural products combretastatins A-1 and A-4 are potent antimitotic and vascular-disrupting agents through their binding at the colchicine site in tubulin. However, these compounds suffer from a low water solubility and a tendency to isomerize to the inactive stilbenes. In this study, we have prepared a series of 18 -restricted triazole analogues of combretastatin A-4 (CA-4), maintaining, in all cases, the 3,4,5-trimethoxy phenyl ring A, with the aim of investigating the substitution pattern on the B-ring in a systematic way.
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