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. 2015 Aug;5(8):388-404.
doi: 10.4172/2161-0444.1000291. Epub 2015 Aug 22.

Diverse Molecular Targets for Chalcones with Varied Bioactivities

Bo Zhou  1 , Chengguo Xing  1
Affiliations

Diverse Molecular Targets for Chalcones with Varied Bioactivities

Bo Zhou et al. Med Chem (Los Angeles). 2015 Aug.

Abstract

Natural or synthetic chalcones with different substituents have revealed a variety of biological activities that may benefit human health. The underlying mechanisms of action, particularly with respect to the direct cellular targets and the modes of interaction with the targets, have not been rigorously characterized, which imposes challenges to structure-guided rational development of therapeutic agents or chemical probes with acceptable target-selectivity profile. This review summarizes literature evidence on chalcones' direct molecular targets in the context of their biological activities.

Keywords: Chalcone; Mechanism of action; Molecular target.

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Figures

Figure 1
Figure 1
A. Structure scaffold of chalcone and examples of bioactivities; B. Examples of chalcones that have been marketed or clinically tested.
Figure 2
Figure 2
Structures of anti-microtubule chalcones.
Figure 3
Figure 3
Structures of chalcones as IKK inhibitors.
Figure 4
Figure 4
Structures of chalcones as Aurora kinase inhibitors.
Figure 5
Figure 5
Structures of chalcones as inhibitors of RTKs.
Figure 6
Figure 6
Structures of chalcones as inhibitors of other kinases.
Figure 7
Figure 7
Structures of chalcones as COX inhibitors.
Figure 8
Figure 8
Structures of chalcones as tyrosinase inhibitors.
Figure 9
Figure 9
Structures of chalcones as inhibitors of sex hormone converting enzymes.
Figure 10
Figure 10
Structures of chalcones as ALR2 inhibitors.
Figure 11
Figure 11
Structures of chalcones as TrxR and MAO inhibitors.
Figure 12
Figure 12
Structures of chalcones as inhibitors of proteases.
Figure 13
Figure 13
Structures of chalcones as HDAC inhibitors.
Figure 14
Figure 14
Structures of chalcones as AChE/BChE inhibitors.
Figure 15
Figure 15
Structures of chalcones as PTP inhibitors.
Figure 16
Figure 16
Figure 16A. Structures of chalcones as sPLA2 inhibitors. Figure 16B. Structures of chalcones as α-glucosidase inhibitors.
Figure 17
Figure 17
Structures of chalcone compounds targeting microbial enzymes.
Figure 18
Figure 18
Structures of chalcone compounds as ligands of various receptors.
Figure 19
Figure 19
Structures of chalcones as inhibitors of ABC transporters.
Figure 20
Figure 20
Structures of chalcones as TOPO inhibitors.
Figure 21
Figure 21
Structures of chalcones acting as MD-2 or MDM2 ligands, or CETP inhibitors.
See this image and copyright information in PMC

References

    1. Batovska DI, Todorova IT. Trends in utilization of the pharmacological potential of chalcones. Curr Clin Pharmacol. 2010;5:1–29. - PubMed
    1. Sahu NK, Balbhadra SS, Choudhary J, Kohli DV. Exploring pharmacological significance of chalcone scaffold: a review. Curr Med Chem. 2012;19:209–225. - PubMed
    1. Singh P, Anand A, Kumar V. Recent developments in biological activities of chalcones: a mini review. Eur J Med Chem. 2014;85:758–777. - PubMed
    1. Karthikeyan C, Moorthy NS, Ramasamy S, Vanam U, Manivannan E, et al. Advances in chalcones with anticancer activities. Recent Pat Anticancer Drug Discov. 2015;10:97–115. - PubMed
    1. Mahapatra DK, Bharti SK, Asati V. Anti-cancer chalcones: Structural and molecular target perspectives. European journal of medicinal chemistry. 2015;98:69–114. - PubMed