Identification of quinoline-chalcones and heterocyclic chalcone-appended quinolines as broad-spectrum pharmacological agents

Abstract

Quinoline derivatives have been reported to possess enticing pharmacological properties. In particular, quinoline-chalcones are identified as promising scaffolds for drug discovery. For a long, the quinoline analogs have been in clinical use for various medical conditions such as cancer inhibitory activity, antibacterial and antifungal, anti-plasmodial, DNA damage inhibitory activity, etc. The number of causalities recorded because of the above-mentioned clinical states is significantly large. Though drug design and discovery is a continuous process all over the world, issues like drug-resistance, low metabolic stability, and long-range side effects are potential hindrances for the continuous use of present pharmacological drugs. In this review work, we focused on the recent drug discovery based on quinoline-chalcones. The work emphasizes the potency of a wide range of quinoline chalcone analogs towards the inhibition of infections caused by the various pathogenic microbes such as bacteria, fungi, plasmodium. Alongside, the quinoline chalcones possessing DNA cleavage properties and cancer cell growth inhibitory properties are also discussed. More importantly, the strongest pharmacological molecules are identified based on the inhibitory properties, cytotoxic values, and pharmacokinetics of synthesized derivatives. Additionally, a structure-activity relationship is established amongst the evaluated molecules. Supplemented by the mechanism of action in few pharmacological activities, the potent activity is also proved by the favorable binding interactions in molecular simulation studies.

Keywords: Anticancer activity; Antifungal & antibacterial activity; Antiprotozoal activity; Quinoline-chalcones; Structure–activity relationship.