Abstract Quinoline is a significant scaffold among heterocyclic compounds and can be used as a key building block for the development of novel medications. Quinoline and its derivatives are recognised as biologically active substances with a number of pharmacological properties. Nowadays, quinoline‐ based heterocycle scaffolds have achieved a prominent position in medicinal chemistry due to their significant pharmacological and biological properties. The discovery and creation of cutting‐edge medications to treat a variety of diseases is an example of the usefulness of these compounds. The current study outlines the range of methods available to create different quinolone‐based heterocycle scaffolds and their advantageous therapeutic applications using the literature that has been published up to 2022.