A twenty-year journey exploring coumarin-based derivatives as bioactive molecules

被引:16
作者
Pisani, Leonardo [1 ]
Catto, Marco [1 ]
Muncipinto, Giovanni [2 ]
Nicolotti, Orazio [1 ]
Carrieri, Antonio [1 ]
Rullo, Mariagrazia [1 ]
Stefanachi, Angela [1 ]
Leonetti, Francesco [1 ]
Altomare, Cosimo [1 ]
机构
[1] Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy
[2] Photys Therapeut, Cambridge, MA USA
来源
FRONTIERS IN CHEMISTRY | 2022年 / 10卷
关键词
cholinesterases; monoamine oxidases; coumarin; neurodegeneration; cancer; MONOAMINE-OXIDASE-B; BIOLOGICAL EVALUATION; 2H-CHROMEN-2-ONE DERIVATIVES; HIGHLY POTENT; INHIBITORS; ACETYLCHOLINESTERASE; DESIGN; SITE; LIPOPHILICITY; DISCOVERY;
D O I
10.3389/fchem.2022.1002547
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The coumarin core (i.e., 1-benzopyran-2 (2H)-one) is a structural motif highly recurrent in both natural products and bioactive molecules. Indeed, depending on the substituents and branching positions around the byciclic core, coumarin-containing compounds have shown diverse pharmacological activities, ranging from anticoagulant activities to anti-inflammatory, antimicrobial, anti-HIV and antitumor effects. In this survey, we have reported the main scientific results of the 20-years investigation on the coumarin core, exploited by the research group headed by Prof. Angelo Carotti (Bari, Italy) either as a scaffold or a pharmacophore moiety in designing novel biologically active small molecules.
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页数:8
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