Journal ArticleDOI
Recent advances and therapeutic journey of coumarins: current status and perspectives
Kuldipsinh P. Barot,Shailesh V. Jain,Laurent Kremer,Laurent Kremer,Shubhra Singh,Shubhra Singh,Shubhra Singh,Manjunath Ghate +7 more
TLDR
The occurence, synthesis and specific biological activities of various coumarin derivatives are described for the discovery and development of new synthetic strategies that could help in structure–activity relationship (SAR) studies.Abstract:
Coumarins are oxygen-containing molecules with specific benzopyrone nucleus. Different coumarins are identified as antineurodegeneratives, anticoagulants, antioxidants, antimicrobials, anticancers, antivirals, antidiabetics, antidepressants, supramoleculars, antiparasitics, anti-inflammatory, analgesics, biological stains, pathological probes and diagnostics. Coumarins have received more attention as compared to 1-azacoumarins. Many attempts have been made for the comparison of both the systems at different stages to discover novel synthetic methodologies, reactivity strategies and biological activities. Translation of current knowledge into novel potent lead compounds and repositioning of well-known compounds for the treatment of different acute and chronic diseases are the current challenges of coumarins. This review article focusses on the occurence, synthesis and specific biological activities of various coumarin derivatives. Some novel research approaches are also described for the discovery and development of new synthetic strategies that could help in structure–activity relationship (SAR) studies. Cellular and molecular mechanisms of coumarins involved in SAR studies are also described.read more
Citations
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Journal ArticleDOI
Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds
TL;DR: 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.
Journal ArticleDOI
An overview of coumarin as a versatile and readily accessible scaffold with broad-ranging biological activities
TL;DR: This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.
Journal ArticleDOI
New Insights into the Antibacterial Activity of Hydroxycoumarins against Ralstonia solanacearum
TL;DR: It is demonstrated that hydroxycoumarins have superior antibacterial activity against the phytopathogen R. solanacearum, and thus have the potential to be applied for controlling plant bacterial wilt.
Journal ArticleDOI
Synthesis of novel coumarin appended bis(formylpyrazole) derivatives: Studies on their antimicrobial and antioxidant activities.
TL;DR: Detailed quantitative structure-activity relationship (QSAR) analysis indicated the molecular parameters that contribute to increased potency of inhibition and would further encourage understanding in employing coumarin pyrazole hybrids as potential antibiotic agents for treating infections caused by pathogenic microbes and fungi.
References
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Journal ArticleDOI
Screening Search for Organic Fluorophores : Syntheses and Fluorescence Properties of 3-Azolyl-7-diethylaminocoumarin Derivatives
TL;DR: 3-azolyl-7-diethylaminocoumarin derivatives were synthesized and showed red shifts with increases of the molar absorptivities and fluorescence intensities, in comparison with those of the corresponding coumarin-oxazole compounds.
Journal ArticleDOI
Discovery of novel osthole derivatives as potential anti-breast cancer treatment.
TL;DR: Interestingly, some derivatives exhibited good inhibition, among them compound 8e was found to be the most potent compound with IC(50) values of 0.24 μM, 0.31 μM against MCF-7 and MDA-MB-231, respectively, which was improved more than 100-folds compared with its parent compound osthole.
Journal ArticleDOI
6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives in a new approach of the treatment of cancer cell invasion and metastasis
I. Kempen,Marc Hemmer,Stéphane Counerotte,Lionel Pochet,Pascal De Tullio,Jean-Michel Foidart,Silvia Blacher,Agnès Noël,Francis Frankenne,Bernard Pirotte +9 more
TL;DR: Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated.
Journal ArticleDOI
Coumarinic derivatives as mechanism-based inhibitors of α-chymotrypsin and human leukocyte elastase
Lionel Pochet,Caroline Doucet,Georges Dive,Johan Wouters,Bernard Masereel,Michèle Reboud-Ravaux,Bernard Pirotte +6 more
TL;DR: Differences in the inhibitory potency expressed by these molecules cannot only be explained by differences in the reactivity of the lactonic carbonyl group toward the nucleophilic attack.
Journal ArticleDOI
Inhibitors of NQO1: Identification of compounds more potent than dicoumarol without associated off-target effects
TL;DR: Evaluating the off-target effects of substituted coumarin-based compounds identified that will be more pharmacologically useful than dicoumarol for probing the function of NQO1 in cells and tissues finds that a number of them generate much less intracellular superoxide and many of them also show a reduced ability to induce apoptosis when compared to dicOUmarol.
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