Recent advances of quinoline‐based small molecules as kinase inhibitors (2020‐2024)

Quinoline‐containing compounds have gained prominence in drug discovery as versatile scaffolds. These compounds have shown promise in the development of kinase inhibitors, which are crucial treatment options used in various cancer cases. This review explores the recent advances from 2020 to 2024 in the design, synthesis, and optimization of quinoline‐based kinase inhibitors, focusing on their role in targeting key kinases, implicated in cancer signaling pathways. Quinoline derivatives exhibit significant inhibitory activity across a broad spectrum of kinases, highlighting their potential to disrupt aberrant signaling that drives tumor growth and progression. Several FDA‐approved quinoline‐containing compounds are utilized in clinical settings as kinase inhibitors, reinforcing their importance and relevance in clinical oncology. This review compiles the pharmacological profiles of these inhibitors spotlighting key compounds that have demonstrated potent inhibitory activities, excellent selectivity profiles, and promising preclinical or clinical outcomes. The review also addresses the challenges associated with their development and discusses future directions for optimizing quinoline‐based kinase inhibitors, such as leveraging advanced drug design techniques, exploring novel targets, and expanding their use in combination therapies. By summarizing recent advancements, this review aims to provide insights into the evolving landscape of quinoline‐based kinase inhibitors and their potential as next‐generation anticancer therapies.