Dysregulation of signal transducer and activator of transcription 3 (STAT3) is implicated in the pathogenesis of various cancers, underscoring its potential as a cancer therapeutic target. In this work, we designed and synthesized a novel series of (E)-2-cyano-3-(4,9-dioxo-4,9-dihydronaphtho[2,3-b]furan-2-yl) derivatives and evaluated their anti-proliferative effects on tumour cells. Among these derivatives, NW16 exhibited remarkable antiproliferative activity against HCT116 cells, with an IC value of 0.
View Article and Find Full Text PDFEur J Med Chem
November 2024
Cytokines play a crucial role in the pathophysiology of autoimmune and inflammatory diseases, with over 50 cytokines undergoing signal transduction through the Signal Transducers and Activators of Transcription (STAT) signaling pathway. Recent studies have solidly confirmed the pivotal role of STATs in autoimmune and inflammatory diseases. Therefore, this review provides a detailed summary of the immunological functions of STATs, focusing on exploring their mechanisms in various autoimmune and inflammatory diseases.
View Article and Find Full Text PDFDiffuse alveolar hemorrhage (DAH) can be caused by various conditions, categorized as autoimmune and non-autoimmune. Immunofactor-mediated vasculitis, such as Wegener granulomatosis, microscopic polyangiitis, Goodpasture syndrome, connective tissue disorders, and antiphospholipid antibody syndrome, are common autoimmune causes. Non-autoimmune factors include infectious or toxic exposures and neoplastic conditions.
View Article and Find Full Text PDFThe signal transducer and activator of transcription 3 (STAT3) has been established as a crucial drug target in the development of antitumor agents. In this study, a series of 21 derivatives of the STAT3 inhibitor napabucasin were designed and synthesized. Through preliminary screening against tumor cell lines, SZ6 emerged as the most potent compound with half maximal inhibitory concentration (IC) values of 46.
View Article and Find Full Text PDFBackground: The increase in antimicrobial resistance leads to complications in treatments, prolonged hospitalization, and increased mortality. Glabridin (GLA) is a hydroxyisoflavan from Glycyrrhiza glabra L. that exhibits multiple pharmacological activities.
View Article and Find Full Text PDFColorectal cancer (CRC) is trending to be a major health problem throughout the world. Therapeutics with dual modes of action have shown latent capacity to create ideal anti-tumor activity. Signal transducer and activator of transcription 3 (STAT3) has been proved to be a potential target for the development of anti-colon cancer drug.
View Article and Find Full Text PDFThe high lethality of infections and the emergence of antibiotic resistance make the development of new antibiotics urgent. Our previous work identified a hit compound () as a novel () dihydrofolate reductase (DHFR) inhibitor. Herein, we analyzed the antimicrobial profile of and performed a comprehensive structure-activity relationship (SAR) assay based on .
View Article and Find Full Text PDFBiochem Pharmacol
January 2024
A novel class of quinoxaline-arylfuran derivatives were designed, synthesized, and preliminarily evaluated for their antiproliferative activities in vitro against several cancer cell lines and normal cells. The representative derivative exerts a potent antiproliferative effect against HeLa cells (IC value of 10.58 μM), through inducing apoptosis and triggering ROS generation and the accumulation of HeLa cells in vitro.
View Article and Find Full Text PDFA series of novel naphthoquinone-furan-2-cyanoacryloyl hybrids were designed; they were synthesized and preliminarily evaluated for their anti-proliferative activities in vitro against several cancer cell lines and normal cells. The most potent compound, , inhibited the proliferation of HeLa cells (IC value of 3.10 ± 0.
View Article and Find Full Text PDFObjective: To investigate the HbA(1c) proportion and mortality rate across diabetic patients with severe hypoglycemia and the risk factors for death.
Methods: All the diabetic patients with severe hypoglycemia were divided into HbA(1c)<6.5% group and HbA(1c)≥6.