Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights

“…Quinoline is an outstanding planar heterocyclic motif playing a distinctive role in anticancer drug discovery. So far, assortments of quinoline-based small molecules have been developed and investigated against numerous biological targets for cancer treatment displaying exquisite outcomes 22–25 . It is worth stressing that plenty of quinoline derivatives provoked their anticancer impact through different mechanisms of action, such as inhibition of DNA repair, tubulin polymerisation, and inhibition of various enzymes implicated in critical cancer cell proliferation prominently kinases enzymes (EGFR, VEGFR, pim-1 kinase, c-Met factor, and PI3K) which stood out as one of the most significant targets implemented in cancer therapy due to their functions in cellular signal transduction 26–30 .…”

Design, Synthesis, and Anticancer Activity Studies of Novel Quinoline-Chalcone Derivatives

“…It has been reported in the literature that the molecular skeleton of chalcone can induce the production of ROS [ 12 , 15 ]. The assay labeling ROS using DCFH-DA probe revealed that compound 12e could effectively induce ROS generation at concentrations as low as 500 nM ( Figure 6 A).…”

“…In fact, chalcone compounds have shown good therapeutic effects and clinical application potential as anticancer drugs for the treatment of human cancers [5][6][7]. In addition, chalcone fragment was also frequently utilized to design novel agents with other anticancer moieties to enhance the biological efficacy by the molecular hybridization strategy [8][9][10][11][12][13][14][15]. 4-Aminochalcone derivative 1 [12] displayed excellent inhibitory activity against NCI-H460, A549, and H1975 cells with IC 50 values of 2.3, 3.2, and 5.7 µM, respectively.…”

“…Additionally, compound 3 could potently inhibit the activity of cellular DHFR and TrxR in HCT-116 cells. [ 1 , 2 , 4 ] Triazolo [1,5- a ] pyrimidine–chalcone derivative 4 [ 15 ] inhibited MGC-803 cells at the nanomolar level (GI 50 = 0.64 μM) and exhibited its anti-proliferative potency via inducing autophagy and increasing ROS level ( Figure 1 ). Therefore, chalcone fragment might be a valuable and core moiety to design anticancer agents.…”

Design, Synthesis and Anticancer Activity Studies of Novel Quinoline-Indole Derivatives

“…Quinolines are a kind of the six membered nitrogen-containing heterocyclic compounds, and quinoline scaffolds are widely considered as the core skeletons of many natural or synthetic bioactive compounds. [3][4][5] Quinoline derivatives exbibit a great variety of biological activities, [3][4][5][6][7][8][9][10][11][12][13][14][15] such as anticancer, [6] anti-human immunodeficiency virus (HIV) [7] and anti-inflammation [8] activities. Quinoline-based protein kinase inhibitors such as Anlotinib [9] (multi-kinase inhibitor), Bosutinib [10] (Src-Abl inhibitor) and Lenvatinib [11] (multi-kinase inhibitor) have been approved for clinical application.…”