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September 5, 2025Open Access

Quinazolines a-Annelated by Five-Membered Heterocycles: Synthesis and Biological Activity

GLG. N. LipunovaInstitute of Organic Synthesis ENEmiliya V. NosovaUral Federal University VCValery N. CharushinUral Federal University

Key Points

Quinazolines annelated by five-membered heterocycles demonstrate various biological activities, including anticancer effects.
Research focuses on quinazolines that target multiple health issues, including antibacterial and anti-inflammatory activities.
Synthesis methods for quinazolines have been comprehensively analyzed, highlighting drug development perspectives.
Recent efforts in medicinal chemistry aim to create effective agents based on azolo[a]quinazolines for therapeutic use.

Abstract

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.

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