A series of novel 3,4-disubstituted pyrazoles were synthesized. The cytotoxicity against U87MG glioma cell line have been investigated in vitro and three of these compounds showed promising inhibitory activity on cell growth with an IC50 lower than 90 microM. AutoDock molecular docking into type I TGF-beta receptor (TGF-beta-RI; PDB: 1py5) has been done for lead optimization of the mentioned compounds as potential TGF-beta-RI1 inhibitors. In particular, 3-aryl-4-amido pyrazole containing long omega-amino-aliphatic chain emerged as a good candidate for further optimization. Entrapment into targetable PEG-based micelles improved growth inhibition IC50 values up to 100 nM and this could lead to a novel drug delivery strategy for treating glioblastoma.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejmech.2010.01.014 | DOI Listing |
Biomater Adv
January 2025
Joint Centre of Translational Medicine, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China; School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325000, China; Zhejiang Engineering Research Center for Tissue Repair Materials, Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325000, China. Electronic address:
The current unavailability of efficient myocardial repair therapies constitutes a significant bottleneck in the clinical management of myocardial infarction (MI). Ginsenoside Rb1 (GRb1) has emerged as a compound with potential benefits in safeguarding myocardial cells and facilitating the regeneration of myocardial tissue. However, its efficacy in treating MI-related ischemic conditions is hampered by its low bioavailability and inadequate angiogenic properties.
View Article and Find Full Text PDFFood Chem
January 2025
Department of Nanotechnology, North-Eastern Hill University (NEHU), Shillong 793022, Meghalaya, India. Electronic address:
In this study, an alginate-chitosan (AL-CS) nanocomplex decorated with vitamin C coated iron oxide nanoparticles (FeO-vit C NPs) was investigated as a novel nanoiron fortification agent. The FeO-vit C NPs decorated on AL-CS nanocomplex underwent comprehensive characterization, including zeta potential, fourier transform infrared spectroscopy, X-ray diffraction, and UV-vis spectroscopy. The transmission electron microscopy (TEM) analysis confirmed the decoration of FeO-vit C NPs on AL-CS nanocomplex.
View Article and Find Full Text PDFFood Chem
December 2024
Key Laboratory of Tea Science of Ministry of Education, Hunan Agricultural University, Changsha, Hunan 410128, China.
Long-term storage of Liupao tea is conducive to improving its flavour and commercial value. Although bacterial communities influence Liupao tea flavour, their impact during storage remains unclear. The aroma compounds and bacterial communities were determined by headspace solid-phase microextraction coupled with gas chromatography-mass spectrometry (HS-SPME-GC-MS) and Illumina Nova6000 analysis.
View Article and Find Full Text PDFFood Chem
December 2024
Department of Food Science and Technology, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. Electronic address:
Atemoya fruit deteriorates rapidly during post-harvest storage. A complete understanding of the metabolic mechanisms underlying this process is crucial for developing effective preservation strategies. Metabolomic approaches combined with machine learning offer new opportunities to identify quality-related biomarkers.
View Article and Find Full Text PDFComput Methods Programs Biomed
January 2025
Shanghai Maritime University, Shanghai 201306, China. Electronic address:
Background And Objective: Inferring large-scale brain networks from functional magnetic resonance imaging (fMRI) provides more detailed and richer connectivity information, which is critical for gaining insight into brain structure and function and for predicting clinical phenotypes. However, as the number of network nodes increases, most existing methods suffer from the following limitations: (1) Traditional shallow models often struggle to estimate large-scale brain networks. (2) Existing deep graph structure learning models rely on downstream tasks and labels.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!