Indazoles are a class of organic heterocyclic compounds, also known as 1,2-diazaindene and benzopyrazole. Indazole is a good bioisomer of phenol, which is more lipophilic than phenol and less prone to phase I and II metabolism. Indazole derivatives have a wide range of biological activities, and it has been confirmed that indazole compounds have anti-tumor, analgesic, anti-inflammatory and other drug activities. Anticancer is the most important application field of indazole drugs. Renal cell carcinoma, solid tumor, nausea and vomiting caused by chemotherapy and leukemia are the main indications of this structural backbone drug.
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.
The molecular structure of cyclobutane has four carbon atoms, and its four carbon atoms are not in the same plane, which is the folded conformation of cyclobutane. Cyclobutane itself is not of commercial or biological interest, but more complex derivatives are important in biology and biotechnology. Currently, nine FDA-approved drugs contain the cyclobutane structure. From the perspective of therapeutic areas, cyclobutyl drugs are mainly distributed in popular areas such as tumors, neurological diseases, infectious diseases, endocrine and metabolic diseases.