Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds

被引：493

作者：

Stefanachi, Angela ^{[1
]}

Leonetti, Francesco ^{[1
]}

Pisani, Leonardo ^{[1
]}

Catto, Marco ^{[1
]}

Carotti, Angelo ^{[1
]}

机构：

[1] Univ Bari Aldo Moro, Dipartimento Farm Sci Farmaco, Via E Orabona 4, I-70125 Bari, Italy

来源：

MOLECULES | 2018年 / 23卷 / 02期

关键词：

coumarin; aromatase inhibitors; cholinesterase inhibitors; monoamine oxidase inhibitors; multitarget ligands; MONOAMINE-OXIDASE-B; SITE ACETYLCHOLINESTERASE INHIBITORS; SOLVENT-FREE SYNTHESIS; ALZHEIMERS-DISEASE; BIOLOGICAL EVALUATION; CHOLINESTERASE-INHIBITORS; SELECTIVE INHIBITORS; MULTITARGET AGENTS; BREAST-CANCER; 2H-CHROMEN-2-ONE DERIVATIVES;

D O I：

10.3390/molecules23020250

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Many naturally occurring substances, traditionally used in popular medicines around the world, contain the coumarin moiety. Coumarin represents a privileged scaffold for medicinal chemists, because of its peculiar physicochemical features, and the versatile and easy synthetic transformation into a large variety of functionalized coumarins. As a consequence, a huge number of coumarin derivatives have been designed, synthesized, and tested to address many pharmacological targets in a selective way, e.g., selective enzyme inhibitors, and more recently, a number of selected targets (multitarget ligands) involved in multifactorial diseases, such as Alzheimer's and Parkinson's diseases. In this review an overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations. The many existing and recent reviews in the field prompted us to make some drastic selections, and therefore, the review is focused on monoamine oxidase, cholinesterase, and aromatase inhibitors, and on multitarget coumarins acting on selected targets of neurodegenerative diseases.

引用

页数：34

共 176 条

[91] Selective estrogen receptor modulators (SERMs): Mechanisms of anticarcinogenesis and drug resistance [J].