This review covers article and patent data obtained mostly within the period 2013–2024 on the synthesis and biological activity of quinazolines a-annelated by five-membered heterocycles. Pyrrolo-, (iso)indolo-, pyrazolo-, indazolo-, (benz)imidazo-, (benz)thiazolo-, and triazolo- aquinazoline systems have shown multiple potential activities against numerous targets. We highlight that most research efforts are directed to design of anticancer, antibacterial, anti-inflammatory, and other agents of azoloaquinazoline nature. This review emphases both the medicinal chemistry aspects of pyrroloa-, (iso)indoloa-, and azoloaquinazolines and the comprehensive synthetic strategies of quinazolines annelated at the N(1)–C(2) bond from the perspective of drug development and discovery.
Lipunova et al. (Wed,) studied this question.