With four imidazopyridine-containing drugs and one pyrazolopyridine-containing drug on the market, bicyclic pyridines containing ring-junction nitrogen are privileged structures in medicinal chemistry. With two nitrogen atoms with potential to serve as hydrogen bond acceptors, imidazopyridines and pyrazolopyridines may boost binding to target proteins and elevate potency. In addition, these structures have found utility in FBDD, covalent inhibitors, reducing metabolic liabilities, and creating novel chemical space and intellectual properties. With many of the advanced intermediates now commercially available, they will find more and more applications in drug discovery.
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Coumarin occurs naturally in a variety of plants, such as lentils, sweet sawdust, vanilla grass, and sweet grass. Coumarin has a simple structure, benzopyrone, associated with different reaction centers. Coumarins are further subdivided into different classes: simple coumarins, pyranocoumarins, furanocoumarins, dicoumarins and isocoumarins. Coumarin derivatives are an important class of natural plant metabolites with various biological activities. They can also be synthesized artificially, and various synthetic coumarin derivatives (azoles, sulfonyls, furans, pyrazoles, etc.) have shown good anticancer, antitumor and antiproliferative activities. Coumarin derivatives are not only effective anticancer agents, but also possess minimum side effects. Based on different substitution patterns, these potential active substances show a great ability to modulate potential anticancer activities.
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