Chalcone hybrids and their antimalarial activity

Abstract

Malaria, one of the most striking, re‐emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug‐resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed.

Chalcone Derivatives: Role in Anticancer Therapy

“…Chalcones, which belong to the flavonoid family and act as intermediates in the biosynthesis of flavonoids, exhibit structural heterogeneity and can act on various drug targets. Chalcone family members have received considerable attention not only because of the possibilities for their synthetic and biosynthetic production but also because of the scope of their biological activities, including anticancer [ 10 ], anti-inflammatory [ 11 ], antidiabetic [ 12 ], cancer chemopreventive [ 13 ], antioxidant [ 14 ], antimicrobial [ 15 ], antileishmanial [ 16 ] and antimalarial activities [ 17 ]. More importantly, several chalcone compounds have been approved for market and clinical use for various health conditions [e.g., as metochalcone-choleretic/diuretics ( 1 ); sofalcone-based anti-ulcer/mucoprotectives ( 2 ); and hesperidin methylchalcone-vascular protectives ( 3 )], exemplifying the clinical potential of chalcones [ 2 , 8 , 9 , 18 ] ( Figure 1 ).…”

Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

“…The simple chemical structure ( Figure 1 ) and a wide range of modifications in their molecules increase the ability of chalcones to affect various molecular and cell signaling targets in the organism [ 8 ]. Plenty of studies have documented numerous biological actions of chalcones including anti-inflammatory [ 16 ], antirheumatic [ 17 ], antidiabetic [ 18 ], antimicrobial [ 19 , 20 , 21 ], immunomodulatory [ 22 ], antimalarial [ 23 ], antiparasitic [ 24 ], and antiproliferative [ 25 , 26 ] effects. Moreover, the anticancer effect of chalcones in experimental animals has also been shown [ 27 , 28 ].…”

The antimalarial activity of indole alkaloids and hybrids

“…Malaria is a deadly parasitic disease caused by five species of malaria parasites Plasmodium falciparum , Plasmodium vivax , Plasmodium malariae , Plasmodium ovale , and Plasmodium knowlesi , and P. falciparum induces the highest malaria mortality. [ 1,2 ] It is estimated by the World Health Organization (WHO) that more than 40% of the world's population lives in areas at risk for malarial transmission, and around 228 million new cases of malaria with 405,000 deaths occurred worldwide in 2018. [ 3 ] Globally, the elimination net is widening, but the situation is increasingly jeopardized by the emergence and spread of P. falciparum strains.…”