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Chalcone: A Privileged Structure in Medicinal Chemistry

Overview
Journal Chem Rev
Specialty Chemistry
Date 2017 May 11
PMID 28488435
Citations 301
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Abstract

Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.

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References
1.
Li H, Zu L, Xie H, Wang J, Jiang W, Wang W . Enantioselective organocatalytic double Michael addition reactions. Org Lett. 2007; 9(9):1833-5. DOI: 10.1021/ol070581y. View

2.
Hara H, Ikeda R, Ninomiya M, Kamiya T, Koketsu M, Adachi T . Newly synthesized 'hidabeni' chalcone derivatives potently suppress LPS-induced NO production via inhibition of STAT1, but not NF-κB, JNK, and p38, pathways in microglia. Biol Pharm Bull. 2014; 37(6):1042-9. DOI: 10.1248/bpb.b14-00116. View

3.
DiCesare N, Lakowicz J . Chalcone-analogue fluorescent prfobes for saccharides signaling using the boronic acid group. Tetrahedron Lett. 2021; 43(14):2615-2618. PMC: 8022852. DOI: 10.1016/s0040-4039(02)00312-x. View

4.
Ziegler S, Pries V, Hedberg C, Waldmann H . Target identification for small bioactive molecules: finding the needle in the haystack. Angew Chem Int Ed Engl. 2013; 52(10):2744-92. DOI: 10.1002/anie.201208749. View

5.
Lounsbury N, Mateo G, Jones B, Papaiahgari S, Thimmulappa R, Teijaro C . Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy. Bioorg Med Chem. 2015; 23(17):5352-9. DOI: 10.1016/j.bmc.2015.07.056. View