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    • Many coumarin derivatives can be found

    2024-04-29

    Many coumarin derivatives can be found in nature. There are more than 1300 types of those purely derived from plants, and if synthetic products are included, their number is immeasurable. According to the earliest existing records extant, herbs containing Psoralen-type compounds, e.g., methoxsalen, were used in the treatment of vitiligo as long ago as 1400 BCE. Among these is one of the most famous coumarin derivatives, warfarin, which is a blood anti-coagulant, and other derivatives are also known to possess a variety of pharmacological characteristics, such as anti-inflammatory, anti-oxidant, anti-viral, anti-bacterial, anti-hyperlipidemic and anti-tumour characteristics., , Moreover, the use of their derivatives goes beyond pharmaceutical applications, for they are also used as fluorescent substances. Additionally, furanocoumarin derivatives are used as drug-metabolizing enzyme inhibitors, and their utility in drug metabolism studies or diagnostics is, among other characteristics, a subject of investigation., Furthermore, it has been reported that coumarin derivatives and inhibit 17β-hydroxysteroid dehydrogenase and steroid sulphatase (STS) (). In recent years, with progress being made in the research of structure–activity relationships using docking studies, structure–activity relationships concerning the anti-tumour characteristic of coumarin derivatives have also been investigated alongside the design of drugs that utilize coumarin at the active site of enzymes. We also conducted studies that focus on coumarin derivatives and reported on the fluorescence characteristics of 7-diethylaminocoumarin analogues that have an Ar group at position 3., We investigated the structure–activity relationship of coumarin and furanocoumarin derivatives with the inhibitory effects of CYP2A6 and CYP3A4., , AI , 17β-hydroxysteroid dehydrogenase inhibitor , and STS inhibitor have a substituent at lactone ring (3 or 4 position) or benzene ring (7 position). Leonetti reported structure-activity relationship study of CYP19 activity and coumarin derivatives having heterocyclic ring at 3–8 position, the optimal position of the hetero ring is 3 or 4 position. We have conducted studies that focus on coumarin derivatives and reported on the fluorescence characteristics of 7-diethylaminocoumarin analogues that have an Ar group at position 3., Thus we have technique synthesis of coumarin derivatives and fluorescent 7-diethylaminocoumarin derivatives having hetero ring at 3 position.
    Introduction Gene Phenyl sulfate and enzyme activity studies have established that aromatase is present in most peripheral organs as well as in the brain of both mammalian and non-mammalian species including fish, birds, rodents, non-human primates and humans (Naftolin et al., 1996, Reviewed in Simpson et al., 2002). In vivo visualization of aromatase only became possible following the development and validation of specific radiopharmaceuticals which, in conjunction with positron emission tomography (PET), could be used to produce three dimensional, quantitative maps of aromatase availability throughout the body. This step was facilitated by the discovery and clinical development of potent and specific drugs designed to inhibit aromatase (aromatase inhibitors, AI), which are increasingly replacing estrogen receptor antagonists in the hormonal treatment of breast cancer (Buzdar and Howell, 2001, Cohen et al., 2002, Howell et al., 2005) with potential use in other cancer and non-cancer indications in both men and women (De Ronde and De Jong, 2011, Fedele et al., 2008, Li et al., 2008). Several aromatase inhibitors, including vorozole ((S)-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole), Ki=0.7nM (Vanden Bossche et al., 1990) letrozole and cetrozole have been labeled with carbon-11 using [11C]-methyl iodide and evaluated as radiotracers for in vivo visualization of aromatase in rodents and primates (Lidstrom et al., 1998, Takahashi et al., 2006, Takahashi et al., 2014, Kim et al., 2009a, Kim et al., 2009b, Kil et al., 2009, Biegon et al., 2010a, Pareto et al., 2013). While letrozole failed to exhibit specific uptake in baboons in vivo (Kil et al., 2009); [11C]vorozole brain scans revealed high specific binding in the rhesus and baboon amygdala, similar to results obtained with autoradiography of the rat brain (Lidstrom et al., 1998, Takahashi et al., 2006, Kim et al., 2009a, Kim et al., 2009b). We have recently reinvestigated and modified the radiosynthesis and purification of [11C]vorozole (Kim et al., 2009a, Kim et al., 2009b). The pure [11C]vorozole was tested and validated in the brains of female baboons and was the first aromatase radiotracer used in human brain studies (Biegon et al., 2010a, Biegon et al., 2010b, Biegon et al., 2015), while both vorozole and cetrozole were used in studies of non-human primates (Lidstrom et al., 1998, Takahashi et al., 2006, Takahashi et al., 2014, Kim et al., 2009a, Kim et al., 2009b). To date, In vivo visualization of aromatase was employed to localize the enzyme in healthy rats, monkeys and human subjects as well as in the context of exposure to drugs and perturbations of homeostasis.