Abstract
Cancer, which can invade and metastasize to almost all organs or tissues, is one of the deadliest diseases across the world. Drug resistance, especially multidrug resistance, is a principal obstacle to effective therapeutic interventions against cancer, creating an urgent demand for the exploration of novel anticancer chemotherapeutics. Quinazoline derivatives are useful templates for exploring new anticancer chemotherapeutics due to their ability to exert anticancer effects through various mechanisms, mainly associated with alterations in cell cycle progression, induction of apoptosis, and modification of autophagy. Moreover, tens of quinazoline-based agents have already been approved for cancer therapy, occupying a prominent place in the current therapeutic arsenal. This review provides an overview of the current status of quinazoline derivatives that hold in vivo anticancer therapeutic potential, along with their mechanisms of action, toxicity profiles, and pharmacokinetic characteristics, encompassing literature published from 2015 to the present.