Cancer is a broad group of diseases that can affect any organ or tissue in the body due to abnormal cellular growth for unknown reasons. Many existing chemotherapeutic agents are highly toxic and have low selectivity. They also contribute to the development of therapeutic resistance. As a result, cancer treatment requires the development of targeted chemotherapeutic agents with low side effects and high selectivity. Quinazoline is a critical scaffold that has been linked to a variety of biological activities. One of the most notable biological activities of this scaffold is its anticancer activity. Several established anticancer quinazolines work on various molecular targets via different mechanisms. The goal of this review is to present various aspects of medicinal chemistry such as drug design, structure-activity relationship, and mode of action of some anticancer quinazoline derivatives. It focuses on the chemotherapeutic activity of quinazolines from the standpoint of drug discovery and development. This review provides medicinal chemists with a bird's-eye view to aid in their efforts to design and synthesise novel quinazolines as targeted chemotherapeutic agents.
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