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Synthesis and Anticancer Properties of ‘Azole’ Based Chemotherapeutics as Emerging Chemical Moieties: A Comprehensive Review

[ Vol. 25 , Issue. 6 ]


Parteek Prasher*, Mousmee Sharma, Flavia Zacconi, Gaurav Gupta, Alaa A.A. Aljabali, Vijay Mishra, Murtaza M. Tambuwala, Deepak N. Kapoor, Poonam Negi, Terezinha de Jesus Andreoli Pinto, Inderbir Singh, Dinesh K. Chellappan and Kamal Dua*   Pages 654 - 668 ( 15 )


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.


Azole, anticancer drugs, chemotherapeutics, molecular inhibitors, anticancer pathways, MAPK, TNF-α, NF-κB.


Department of Chemistry, University of Petroleum & Energy Studies, Dehradun 248007, Department of Chemistry, Uttaranchal University, Arcadia Grant, Dehradun 248007, Departamento de Quimica Organica, Facultad de Quimica y de Farmacia, Pontificia Universidad Catolica de Chile, Av. Vicuna Mackenna 4860, Macul, Santiago 7820436, School of Pharmacy, Suresh Gyan Vihar University, Jagatpura 302 017, Jaipur, Faculty of Pharmacy, Department of Pharmaceutics and Pharmaceutical Technology, Yarmouk University, Irbid, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, School of Pharmacy and Pharmaceutical Science, Ulster University, Coleraine, County Londonderry, Northern Ireland BT52 1SA, School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Post box no. 9, Solan, Himachal Pradesh 173 229, School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Post box no. 9, Solan, Himachal Pradesh 173 229, Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Street, São Paulo 05508-000, Chitkara College of Pharmacy, Chitkara University, Punjab, 140401, Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur 57000, Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW 2007

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