Exploring Quinolone Scaffold: Unravelling the Chemistry of Anticancer Drug Design

Abstract

: Globally, cancer is considered as the major leading cause in decreasing the patient health care system of human beings. The growing threat from drug-resistant cancers makes heterocyclic moieties as an urgent need to develop more successful candidates for anti-cancer therapy. In view of outstanding pharmacological activities Quinolone and its derivatives have attracted more attention towards drug designing and biological evaluation in the search of new drug molecules. The inspired researchers attempted efforts in order to discover quinolone based analogs due to its wide range of biological activities. Due to immense pharmacological importance, distinct synthetic methods have been executed to attain new drug entities from quinolones and all the reported molecules have shown constructive anticancer activity. Some of the synthetic protocol like, one pot synthesis, post-Ugi-transformation, catalysed based synthesis, enzyme-based synthesis and nano-catalyst based synthetic procedures are also discussed as recent advancement in production of quinolone derivatives. In this review, recent synthetic approaches in the medicinal chemistry of quinolones and potent quinolone derivatives on the basis of structural activity relationship are outlined. Moreover, their major methods and modifications are discussed.

DNA Gyrase as a Target for Quinolones

“…Various research and review articles have been published on quinolones and their antibacterial, as well as other biological properties [49,50]. The previous review articles were focused either on antimicrobial drugs/molecules with different targets [51][52][53][54][55], or molecules effective against a specific target, such as protein synthesis [56,57], cell wall [58,59], and DNA gyrase [60][61][62][63]. Although many have covered the breadth needed as well as the importance of quinolones in drug discovery [64][65][66][67][68], we could not locate any reports which exclusively focus on the DNA gyrase inhibitory properties of quinolone and the detailed insights.…”