Synthesis and anticancer properties of 'azole'based chemotherapeutics as emerging chemical moieties: A comprehensive review

Parteek Prasher, Mousmee Sharma, Flavia Zacconi, Gaurav Gupta, Alaa A. Aljabali, Vijay Mishra, Murtaza M. Tambuwala, Deepak N. Kapoor, Poonam Negi, Terezinha De Jesus Andreoli Pinto, Inderbir Singh, Dinesh Kumar Chellappan, Kamal Dua

Research output: Contribution to journalArticlepeer-review

20 Citations (Scopus)
9 Downloads (Pure)


Azole frameworks serve as privileged scaffolds in the contemporary drug design paradigm owing to their unique physicochemical profile that promotes the development of highly selective, physiological benevolent chemotherapeutics. Several azole nuclei function as bioisostere in medicinal chemistry and prompt the development of tailored therapeutics for targeting the desired biological entities. Besides, the azole scaffold forms an integral part in the advanced drug designing methodologies, such as target template insitu drug synthesis, that assists in rapid identification of the hit molecules form a diverse pool of leads; and direct biomolecule-drug conjugation, along with bioorthogonal strategies that ensure localization, and superior target specificity of the directed therapeutic. Lastly, the structural diversity of azole framework and high yielding click synthetic methods provide a comprehensive Structure-Activity Relationship analysis for design optimization of the potential drug molecules by fine-tuning the placement of different substituents critical for the activity. This review provides a comprehensive analysis of the synthesis and anticancer potential of azole based chemotherapeutics.
Original languageEnglish
Pages (from-to)654-668
Number of pages15
JournalCurrent Organic Chemistry
Issue number6
Publication statusPublished (in print/issue) - 20 Aug 2020


  • Organic Chemistry


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