A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and (1)H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46±0.008 and 312.79±0.06 μM when compared with the standard acarbose (IC50, 38.25±0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46±0.008, 37.78±0.05, 28.91±0.0, 38.12±0.04, 37.43±0.03, 36.89±0.06 and 37.11±0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bioorg.2014.12.001 | DOI Listing |
Cancer Med
March 2025
Institute of Microcirculation, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, China.
Background: Tumor metastasis is one of the main causes of death in cancer patients; however, the mechanism controlling metastasis is unclear. The posttranscriptional regulation of metastasis-related genes mediated by AT-rich interactive domain-containing protein 4A (Arid4a), an RNA-binding protein (RBP), has not been elucidated.
Methods: Bioinformatic analysis, qRT-PCR, immunohistochemistry, and immunoblotting were employed to determine the expression of Arid4a in breast tumor tissues and its association with the survival of cancer patients.
Front Immunol
March 2025
Department of Orthopedics, The Second Affiliated Hospital of Nanchang University, Nanchang, Jiangxi, China.
Background: Osteosarcoma, an aggressive bone malignancy predominantly affecting children and adolescents, presents significant therapeutic challenges with a 5-year survival rate below 30% in metastatic cases. T-cell exhaustion, characterized by the overexpression of immune checkpoint molecules, contributes to osteosarcoma progression and immune evasion. Although targeting these inhibitory pathways has shown potential in restoring T-cell activity, the molecular regulators of T-cell depletion in osteosarcoma are poorly understood.
View Article and Find Full Text PDFFront Microbiol
February 2025
Department of Pharmacy, Mie University Hospital, Mie, Japan.
Introduction: Isavuconazole, a broad-spectrum triazole approved by the United States Food and Drug Administration (FDA) in 2015, moderately inhibits cytochrome P450 3A4. Although antifungal agents are often used concomitantly with cyclosporine, the effect of switching from voriconazole to isavuconazole on the blood cyclosporine level remains unclear.
Case: A 63-year-old Japanese male was administered oral cyclosporine (10:00 and 21:00) for severe aplastic anemia.
Iran J Pharm Res
December 2024
Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Background: is a significant contributor to a range of gastrointestinal conditions, with conventional treatment methods primarily relying on antibiotics. However, the rise of antibiotic-resistant strains has necessitated the exploration of alternative therapeutic approaches.
Objectives: To determine the antibacterial potential of probiotic bacteria ( BLRH 260 and ) and four propolis extracts against and to analyze their impacts on body weight index and histopathological changes in -challenged Wistar rats.
Heliyon
February 2025
São Paulo State University (UNESP), School of Dentistry, Araraquara, SP, Brazil.
The growing global threat posed by microorganisms resistant to conventional antimicrobials underscores the urgent need for novel agents to control infections. The aim of this study was to evaluate the antimicrobial activity and biocompatibility of alpha-silver tungstate (α-AgWO) nanoparticles (NPs) synthesized by the ultrasonic method. The NPs were characterized, and their antimicrobial activity was assessed against , , and using the broth microdilution method, determining the minimum inhibitory concentration (MIC) and minimum bactericidal/fungicidal concentration (MBC/MFC).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!