1. Academic Validation
  2. Quinazolines annelated at the N(3)-C(4) bond: Synthesis and biological activity

Quinazolines annelated at the N(3)-C(4) bond: Synthesis and biological activity

  • Eur J Med Chem. 2024 May 5:271:116411. doi: 10.1016/j.ejmech.2024.116411.
Emiliya V Nosova 1 Galina N Lipunova 2 Yulia V Permyakova 3 Valery N Charushin 4
Affiliations

Affiliations

  • 1 Department of Organic and Biomolecular Chemistry, Ural Federal University, 19 Mira st., Ekaterinburg, 620002, Russia; Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22 S. Kovalevskaya st. /20 Akademicheskaya st., Ekaterinburg, 620137, Russia. Electronic address: [email protected].
  • 2 Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22 S. Kovalevskaya st. /20 Akademicheskaya st., Ekaterinburg, 620137, Russia. Electronic address: [email protected].
  • 3 Department of Organic and Biomolecular Chemistry, Ural Federal University, 19 Mira st., Ekaterinburg, 620002, Russia.
  • 4 Department of Organic and Biomolecular Chemistry, Ural Federal University, 19 Mira st., Ekaterinburg, 620002, Russia; Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22 S. Kovalevskaya st. /20 Akademicheskaya st., Ekaterinburg, 620137, Russia.
Abstract

This review covers article and patent data obtained mostly within the period 2013-2023 on the synthesis and biological activity of quinazolines [c]-annelated by five- and six-membered heterocycles. Pyrazolo-, benzimidazo-, triazolo- and pyrimido- [c]quinazoline systems have shown multiple potential activities against numerous targets. We highlight that most research efforts are directed to design of Anticancer and Antibacterial agents of azolo[c]quinazoline nature. This review emphases both on the medicinal chemistry aspects of pyrrolo[c]-, azolo[c]- and azino[c]quinazolines and comprehensive synthetic strategies of quinazolines annelated at N(3)-C(4) bond in the perspective of drug development and discovery.

Keywords

Advanced synthesis; Azinoquinazolines; Azoloquinazolines; Biological activity; Indoloquinazolines.

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