Lipunova Galina N, Nosova Emiliya V, Charushin Valery N
Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22 S. Kovalevskaya St./20 Akademicheskaya St., Ekaterinburg 620137, Russia.
Department of Organic and Biomolecular Chemistry, Ural Federal University, 19 Mira St., Ekaterinburg 620002, Russia.
Molecules. 2025 Aug 27;30(17):3506. doi: 10.3390/molecules30173506.
This review covers article and patent data obtained mostly within the period 2013-2024 on the synthesis and biological activity of quinazolines []-annelated by five-membered heterocycles. Pyrrolo-, (iso)indolo-, pyrazolo-, indazolo-, (benz)imidazo-, (benz)thiazolo-, and triazolo- []quinazoline 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 azolo[]quinazoline nature. This review emphases both the medicinal chemistry aspects of pyrrolo[]-, (iso)indolo[]-, and azolo[]quinazolines and the comprehensive synthetic strategies of quinazolines annelated at the N(1)-C(2) bond from the perspective of drug development and discovery.
本综述涵盖了主要在2013年至2024年期间获得的关于五元杂环稠合喹唑啉的合成及生物活性的文章和专利数据。吡咯并、（异）吲哚并、吡唑并、吲唑、（苯并）咪唑、（苯并）噻唑和三唑并喹唑啉系统已显示出针对众多靶点的多种潜在活性。我们强调，大多数研究工作都致力于设计具有唑并喹唑啉性质的抗癌、抗菌、抗炎和其他药物。本综述既强调了吡咯并、（异）吲哚并和唑并喹唑啉的药物化学方面，也从药物开发和发现的角度阐述了在N(1)-C(2)键处稠合喹唑啉的综合合成策略。
