Report on Recently (2017–20) Designed Quinoline‐Based Human Cancer Cell Growth Inhibitors

Abstract

Quinoline has been a most essential pharmacophore, derivatization of which led to enticing pharmacological properties. Quinoline is responsible for a wide range of biological potencies such as antibacterial, antifungal, anti-leishmanial, antimalarial, antioxidant and anticancer properties. Out of these clinical importances, the anticancer property of heterocycles is of greatest concern as cancer has become a major threat globally. Since some natural products containing quinoline moiety have displayed cancer inhibition potency, quinoline has been given highest priority in the anticancer drug design and development. In addition, quinoline has got eight positions including nitrogen for substitution which may result in some potential anticancer properties. Ever since, this extraordinary potential is being utilized in anticancer drug discovery. In this review, the various trends in drug design of quinoline moiety anticipating finest anticancer properties through cancer cell growth inhibition are collated comprehensively. The review work is classified based on type of quinoline derivatives. Besides this, with the aid of structure-activity relationship discussion, the importance of structural units that contributed to strongest activity towards cancer inhibition is emphasized. The particular activity would help to bring further advanced anticancer agents in the future.

Turning a Quinoline-based Steroidal Anticancer Agent into Fluorescent Dye for its Tracking by Cell Imaging

“…Having a quinoline pharmacophore on aminosteroid RM-581, we were interested in turning our anticancer agent into a fluorescent one (RM-581-Fluo; Figure ) by adding a small dimethyl amino group and using this opportunity to provide a new tool for RM-581 MoA studies. Also, considering the large number of quinoline-based anticancer agents, − a successful result could offer a relevant example for the use of such a fluorophore to support biological studies related to this class of pharmaceutical compounds.…”

Autophagic and apoptotic cell death induced by the quinoline derivative 2‐(6‐methoxynaphthalen‐2‐yl)quinolin‐4‐amine in pancreatic cancer cells is via ER stress and inhibition of Akt/mTOR signaling pathway

“…Quinoline core is a significant family of heterocyclic compounds that displays a broad spectrum of pharmacological properties, including anti‐malarial, antimicrobial, antioxidant, anti‐inflammatory, anticancer activity, and so on (Jain et al, 2019; Matada et al, 2021). Many quinoline derivatives have been synthesized and evaluated as anticancer agents (Dorababu, 2020; Hamdy et al, 2019; Kumar et al, 2015; Ma et al, 2019). Some quinoline‐containing drugs with high efficacy are being studied in clinical trials, including Neratinib, Lenvatinib, and Foretinib (Matada et al, 2021).…”

Recent Advances in Transition-Metal-Free Late-Stage C-H and N-H Arylation of Heteroarenes Using Diaryliodonium Salts

“…The arylation was found to be tolerant of various substituted substrates in moderate to good yields depending on the heteroarene. This late-stage C-2 arylation of these essential pharmacophores provided a practical strategy for the synthesis of attractive N -heterobiaryl derivatives that are widely found in pharmaceuticals and natural compounds, particularly in alkaloids [ 77 , 78 , 79 , 80 , 81 ].…”