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.
Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
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