Pyrimidine, also known as 1,3-diazobenzene, is a heterocyclic compound with the chemical formula C4H4N2. Pyrimidine is formed by substituting 2 nitrogen atoms for 2 carbons in the meta-position of benzene. It is a diazine and retains its aromaticity. Derivatives of pyrimidine widely exist in organic macromolecular nucleic acids, and many drugs also contain pyrimidine rings. In nucleic acids, three nucleobases are pyrimidine derivatives: cytosine, thymine and uracil. There are a variety of pyrimidine-containing drugs on the market, most of which are kinase inhibitors.
Fluorine is the most electronegative element in the periodic table, and the fluorine atom has a small atomic radius, so fluorine-containing organic compounds have many wonderful properties. For example, the introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the permeability to cell membranes, metabolic stability and bioavailability; in addition, the introduction of fluorine atoms will improve the lipid solubility of the compound and promote its absorption in the body. The speed of delivery changes the physiological effect. In the field of medicinal chemistry, the introduction of fluorine atoms into organic molecules is an important direction for the development of new anticancer drugs, antitumor drugs, antiviral agents, anti-inflammatory drugs, and central nervous system drugs.
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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