Over the past two decades, small molecules bearing [5,6]-bicyclic nitrogen-containing cores have emerged as one of the most extensively studied structures for the development of selective c-MET kinase inhibitors. Structure-activity relationship (SAR) studies have demonstrated that modifying these cores can significantly impact the biological properties of c-MET inhibitors, including safety/toxicity, potency, and metabolic stability. For example, although c-MET kinase inhibitors containing the [1,2,4]triazolo[4,3-b][1,2,4]triazine scaffold (core P) exhibit high inhibitory potency, they often face challenges due to metabolic stability defects.
View Article and Find Full Text PDFMelatonin, a hormone primarily produced by the pineal gland, exhibits a range of physiological functions that extend beyond its well-known role in regulating circadian rhythms. This hormone influences energy metabolism, modulates insulin sensitivity, and plays a significant role in controlling sleep patterns and food intake. Notably, melatonin is also synthesized in various peripheral organs, including the gastrointestinal system and pancreas, suggesting its function as a local hormone.
View Article and Find Full Text PDFQuercetin, a natural flavonoid, has been extensively researched for its potential in promoting bone regeneration and tissue engineering. This review aimed to provide a comprehensive overview of the applications of quercetin-based biomaterials in bone regeneration and tissue engineering. The review discusses several studies that have integrated quercetin into biomaterials such as electrospun fibers, hydrogels, microspheres, and nanoparticles.
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