Aurones are very simple, promising anticancer lead molecules containing three rings (A, B and C). A very slight structural variation in the aurones elicits diverse affinity and specificity towards different molecular targets. The present review discusses the design, discovery and development of natural and synthetic aurones as small molecule anticancer agents. Detailed structure-activity relationship and intermolecular interactions at different targets are also discussed. Due to their rare occurrence in nature and minimal mention in literature, the anticancer potential of aurones is rather recent but in constant progress.
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http://dx.doi.org/10.1016/j.ejmech.2019.01.078 | DOI Listing |
Sci Rep
December 2024
School of Biological Engineering, Henan University of Technology, No. 100 Lianhua Street, Zhengzhou High-Tech Development Zone, Zhengzhou, 450001, Henan, People's Republic of China.
J Org Chem
September 2024
State Key Laboratory of Chemical Resources Engineering, Beijing University of Chemical Technology, Beijing 100029, China.
Dihydroaurones, which are derivatives of aurones, exhibit similar biological activity. Although there are many synthetic methods for dihydroaurones, ecofriendly methodologies that circumvent the use of precious metals still need to be explored. In this work, a catalyst-free, visible-light-driven synthesis of dihydroaurones has been developed through the cyclization of aromatic diazo compounds.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
December 2024
School of Materials Science and Engineering, University of Jinan, Jinan, China. Electronic address:
To synthesize aurone (Ar) derivatives and to demonstrate their effects against diabetes mellitus (DM) and neurodegeneration. Five Ar () derivatives were synthesized, characterized by proton NMR and screened for antioxidant, anti-diabetic and anti-cholinesterase activities. They were further evaluated for neuroprotective effects in streptozotocin (STZ)-induced neurodegenerative model.
View Article and Find Full Text PDFMolecules
June 2024
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Viale delle Scienze, Ed. 17, I-90128 Palermo, Italy.
Aurones, particular polyphenolic compounds belonging to the class of minor flavonoids and overlooked for a long time, have gained significative attention in medicinal chemistry in recent years. Indeed, considering their unique and outstanding biological properties, they stand out as an intriguing reservoir of new potential lead compounds in the drug discovery context. Nevertheless, several physicochemical, pharmacokinetic, and pharmacodynamic (P3) issues hinder their progression in more advanced phases of the drug discovery pipeline, making lead optimization campaigns necessary.
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