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A twenty-year journey exploring coumarin-based derivatives as bioactive molecules
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Muncipinto, Giovanni
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Photys Therapeut, Cambridge, MA USA Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy

Nicolotti, Orazio
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Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy

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Rullo, Mariagrazia
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Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy

Stefanachi, Angela
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Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy

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Altomare, Cosimo
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Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy Univ Bari Aldo Moro, Dept Pharm Pharmaceut Sci, Bari, Italy
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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