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Published on: February 15, 2016
Quinazolines [a]-Annelated by Five-Membered Heterocycles: Synthesis and Biological Activity
Galina N Lipunova1, Emiliya V Nosova1,2, Valery N Charushin1,2
1Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22 S. Kovalevskaya St./20 Akademicheskaya St., Ekaterinburg 620137, Russia.
None:
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- [a]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[a]quinazoline nature. This review emphases both the medicinal chemistry aspects of pyrrolo[a]-, (iso)indolo[a]-, and azolo[a]quinazolines 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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