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VOL. 9, ISSUE 2 (2025)
Heterocyclic Carboxamides: A strategic review on the Anticancer Potential of Tetrazole and Triazole motifs in drug discovery
Authors
Sushil Eknathrao Jamale, Dr Suresh Govardhan Vedpatahk
Abstract
The enduring challenge of cancer and the rise
of drug resistance necessitate the continuous discovery of novel, selective
therapeutic agents. This review critically assesses the crucial role of
heterocyclic carboxamide scaffolds, focusing specifically on the fusion of the
carboxamide functional group with the nitrogen-rich tetrazole and triazole
motifs, in contemporary anticancer drug development. The carboxamide group is
highlighted as a versatile pharmacophore providing essential hydrogen-bonding
and conformational control. The review details how the tetrazole ring acts as a
potent carboxylic acid bioisostere in targeted agents like VEGFR-2 kinase
inhibitors, while the 1,2,3-triazole ring, predominantly formed through
high-yielding Click Chemistry, serves as a rigid, metabolically stable linker
in compounds targeting HDACs and tubulin polymerization. Key structure-activity
relationships (SAR) are summarized, organized by biological mechanism.
Furthermore, we discuss the advanced methodologies—including High-Throughput
Screening (HTS) and computational modeling (3D-QSAR)—that are accelerating
compound optimization and target validation. Finally, we address persistent
challenges such as poor bioavailability and off-target toxicity, concluding
that integrating sophisticated computational design with synthetic flexibility
will be essential for translating these potent preclinical hits into clinically
viable therapeutics.
Pages:79-84
How to cite this article:
Sushil Eknathrao Jamale, Dr Suresh Govardhan Vedpatahk "Heterocyclic Carboxamides: A strategic review on the Anticancer Potential of Tetrazole and Triazole motifs in drug discovery". International Journal of Chemical Science, Vol 9, Issue 2, 2025, Pages 79-84
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