Chalcones bearing N, O, and S-heterocycles: Recent notes on their biological significances

Abstract

Because of its relatively easy synthesis, chalcone skeleton has been as a point of interest for organic and medicinal chemists from research groups worldwide. Chalcone scaffold constitutes the core of some interesting biologically active natural products. Chalcone derivatives are among feasible potent active agents, such as anticancer, antibacterial, antifungal, antileishmanial, antimalarial, and antiviral. Due to the knowledge of heterocyclic chemistry, recently chalcones bearing heterocyclic moieties have been synthesized and biologically investigated for specific target of diseases. The current review focuses on the latest application of chalcones integrated with N, O, and S-heterocyclic system and their wide spectrum of biological performance during 10 years (2010)(2011)(2012)(2013)(2014)(2015)(2016)(2017)(2018)(2019). The results reported in the review indicate that many chalcone-heterocycle hybrids may be useful as future drug candidates due to their comparable or higher activity than that of the standards.

In silico toxicity prediction, synthesis, characterization, antimicrobial and antioxidant activity of different di substituted chalcones

“…The control sample was prepared using the same volume without any compound and BHT, 95% methanol served as blank. Test was performed in triplicate and the results were averaged [32][33][34][35][36]. Radical scavenging activity was calculated using the formula:…”

Synthesis and Pharmacological Activities of Chalcone and Its Derivatives Bearing N-Heterocyclic Scaffolds: A Review

“…On top of this, many researchers are exhaustively devoted to synthesizing a chalcone derivative incorporating a heterocyclic scaffold. Chalcones incorporating heterocyclic scaffolds have been reported with various biological and pharmacological activities, such as antioxidant activity, 12 antibacterial activity, 12 antifungal activity, 13 antileishmanial activity, 14 anti-inflamatory activity, 15 anticancer activity, 16 antitubercular activity, 17 antiproliferative agents, 17 antimalarial activity, 18 antiplatelet activity, 19 carbonic anhydrase inhibitors, 20 an inhibitor of microsomalenzyme glutathione- S -transferases, 21 and CYP1 enzyme inhibitors. 22 …”

Advances in the Synthesis of Heteroaromatic Hybrid Chalcones

“…The utility of chalcones both as a pharmacophore and as a scaffold in the synthesis of a wide variety of heterocycles ranging from pyrazoles, isoxazoles, triazoles, barbituric acid derivatives, etc. has been investigated thoroughly over the years, with numerous research articles as well as several reviews appearing in the last decade describing the current chalcone synthetic strategies, the heterocycles derived from them, and the bioactivity and pharmaceutical uses of these compounds [ 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 , 13 ]. Within that context, the preparation of more highly functionalized chalcones that contain heteroaromatic components has been an area of intense research over the last decade [ 10 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 ].…”

“…Research has established that heteroaromatic hybrid chalcones themselves possess broad medicinal value as anticancer [ 16 , 19 , 23 ], antimicrobial [ 11 , 20 , 23 , 28 ], antifungal [ 16 ], anti-tuberculosis [ 25 ] and anti-inflammatory agents [ 22 ] as well as having other important pharmacological functions [ 9 , 10 ], agrochemical utility as photosynthesis inhibitors [ 18 ] and industrial use as photoinitiators in 3D printing [ 17 ]. Figure 2 shows a representative selection of heteroaromatic hybrid chalcone pharmacophores and industrially important compounds.…”