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Discovery of -Trifluoromethylated Noscapines as Novel and Potent Agents for the Treatment of Glioblastoma.
J Med Chem
January 2025
Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
The search for new and effective chemotherapeutic agents for the treatment of glioblastoma (GBM) represents an unmet need in drug discovery. Herein, a class of novel -trifluoromethylated noscapines has been disclosed. Among them, 9'-bromo--trifluoromethyl noscapine displayed superior anti-GBM potency.
View Article and Find Full Text PDFEnhanced Bioactivity of Quercetin-Tetrahydroisoquinoline Derivatives: Effect on Lipophilicity, Enzymes Inhibition, Antioxidant Potential, and Cytotoxicity.
Int J Mol Sci
December 2024
Vinča Institute of Nuclear Sciences, National Institute of the Republic of Serbia, University of Belgrade, P.O. Box 522, 11000 Belgrade, Serbia.
Quercetin, a well-known flavonoid with significant medicinal potential, was derivatized at the C8 position with a tetrahydroisoquinoline (THIQ) moiety, and physicochemical and pharmacological properties, inhibition potential, antioxidant activity, and cytotoxicity of new compounds were evaluated. Physicochemical and pharmacological properties, including lipophilicity, membrane permeability, and P-glycoprotein substrate affinity, were assessed theoretically using the SwissADME software. The metal-chelating ability of the new compounds was evaluated on metal ions Fe, Zn, and Cu, whose homeostasis disruption is linked to the development of Alzheimer's disease.
View Article and Find Full Text PDFTrabectedin for L-Type Sarcoma: A Retrospective Multicenter Study.
Curr Oncol
November 2024
Department of Medical Oncology, Ege University Tilay Aktaş Oncology Hospital, 35100 Izmir, Türkiye.
(1) Background: Metastatic L-type sarcomas (liposarcoma and leiomyosarcoma) are rare and have a poor prognosis. Trabectedin is an effective agent that can be used after anthracyclines. This study was designed to evaluate the real-life effectiveness and safety of trabectedin.
View Article and Find Full Text PDFMechanism of efficacy of trabectedin against myxoid liposarcoma entails detachment of the FUS-DDIT3 transcription factor from its DNA binding sites.
J Exp Clin Cancer Res
November 2024
Department of Experimental Oncology, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Milan, Italy.
Background: The marine drug trabectedin has shown unusual effectiveness in the treatment of myxoid liposarcoma (MLPS), a liposarcoma characterized by the expression of the FUS-DDIT3 chimera. Trabectedin elicits a significant transcriptional response in MLPS resulting in cellular depletion and reactivation of adipogenesis. However, the role of the chimeric protein in the mechanism of action of the drug is not entirely understood.
View Article and Find Full Text PDFObjective: The purpose of this study was to evaluate the effectiveness of the drugs Solifenacin and Vesusten in relation to the treatment of neurogenic bladder overactivity in multiple sclerosis (MS).
Materials And Methods: A prospective, single-site, single-center, placebo-controlled, parallel-group, comparative clinical trial was conducted. The study included 41 MS patients of both sexes aged 18-50 years with urodynamically confirmed detrusor overactivity.
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