The current landscape of quinazoline derivatives with in vivo anticancer therapeutic potential-part I.

Abstract

With the development of new technology, cancer has already transformed from a catastrophic disease to a treatable and sometimes curable disease. Chemotherapeutics is critical for cancer therapy, but multidrug resistance and severe side effects often lead to treatment failure, creating an urgent demand to develop innovative and efficient therapeutic interventions. Quinazoline hybrids could arrest the cell cycle, induce apoptosis, inhibit angiogenesis, and disrupt cell migration. Moreover, several quinazoline hybrids, exemplified by Fruquintinib (quinazoline-benzofuran hybrid) and Barasertib (quinazoline-pyrazole hybrid), have already been applied in clinics for cancer therapy, indicating that the rational design of quinazoline hybrids may provide valuable chemotherapeutics for cancer therapy. This review outlines the current scenario of the in vivo anticancer therapeutic potential of quinazoline hybrids, together with modes of action, toxicity, and pharmacokinetic properties, developed from 2015 onwards, aiming to provide promising candidates for further preclinical/clinical evaluations and to facilitate further rational design.