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