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Synthetic approaches for novel fused pyrimidine derivatives: Design, structural characterization, antiviral, antitumor, and molecular docking evaluation.
Heliyon
December 2024
Department of Biology, College of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.
The goal of this work was to synthesize new compounds for anticancer evaluation as a trial to obtain new antitumor agents with higher activity and fewer side effects. Therefore, the precursor 2,2'-(1,4-phenylenebis (thiazole-4,2-diyl))bis (3-(dimethylamino)acrylonitrile) was used to synthesize various azolopyrimidine derivatives connected to the thiazole moiety. Compounds -, including pyrazolopyrimidine, triazolopyrimidine, and others, were produced by reacting enaminonitrile with different -nucleophiles.
View Article and Find Full Text PDFNew thiadiazolopyrimidine-ornamented pyrazolones as prospective anticancer candidates via suppressing VEGFR-2/PI3K/Akt signaling pathway: Synthesis, characterization, in-silico, and in-vitro studies.
Int J Biol Macromol
December 2024
Organic Chemistry, Chemistry Department, Faculty of Science, Tanta University, Tanta 31527, Egypt. Electronic address:
New thiadiazolopyrimidine-ornamented pyrazolones (4a-8b) have been synthesized by a cyclocondensation reaction of 3a, b with different active methylene compounds. The structure of our products was confirmed via different physical and spectroscopic data. We assessed all newly thiadiazolopyrimidine-ornamented pyrazolones' potential to inhibit angiogenesis, metastasis, and cancer growth by utilizing in-silico investigations focused on the VEGFR-2 signaling pathway and elucidate their pharmacokinetic features using ADMET.
View Article and Find Full Text PDFEdaravone's Safety Profile in Acute Ischemic Stroke.
Brain Behav
December 2024
Department of Neurology, Zeenat Qureshi Stroke Institute, Jose R. Reyes Memorial Medical Center, Manila, Philippines.
Background: We aimed to evaluate the safety of intravenous edaravone for the treatment of acute ischemic stroke among Filipino patients. The study, categorized as Phase IV, spans from December 2022 to November 2023. The primary objective is to document side effects and serious adverse events during the 14-day edaravone infusion period.
View Article and Find Full Text PDFEdaravone Protects Trophoblast Cells From Hypoxic Injury in Preeclampsia: Inhibition of the PI3K/AKT Pathway as a Promising Therapeutic Approach.
Immun Inflamm Dis
December 2024
Department of Nuclear Medicine, General Hospital of Northern Theater Command, Shenyang, Liaoning, China.
Objective: Preeclampsia (PE) is a multifaceted medical condition that manifests during pregnancy, characterized by hypertension and damage to multiple organs. In PE, the placenta's impaired functionality leads to continuous hypoxia in placental tissues, which is considered the primary cause of the condition. Inhibition of hypoxia-induced injury in trophoblast cells presents a potential therapeutic strategy for PE.
View Article and Find Full Text PDFEdaravone promotes motoneuron survival and functional recovery after brachial plexus root avulsion and reimplantation in rats: Involvement of SIRT1/TFEB pathway.
Int Immunopharmacol
January 2025
Research Center of Basic Integrative Medicine, School of Basic Medical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China; Department of Medical Biotechnology, School of Basic Medical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China; Dongguan Institute of Guangzhou University of Chinese Medicine, Dongguan, 523808, China. Electronic address:
Background: Brachial plexu root avulsion (BPRA) commonly causes extensive motoneuron death, motor axon degeneration and denervation of biceps, leading to devastating motor dysfunction in the upper limb. Edaravone (Eda) has been proven to exert anti-oxidative and neuroprotective effects on various neurological disorders. Herein, we aimed to investigate the efficacy profile and potential mechanisms of Eda on BPRA in vitro and in vivo models.
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