Introduction: Triazole moiety is considered as the most important heterocyclic therapeutic agent in medicinal chemistry. Identifying a lead compound or potential drug, with the requisite physical and biological characteristics from a library of known bioactive molecules is the first step in the traditional drug development process which involves identifying the protein target associated with the disease. This severely restricts the search space from the outset and makes the task of discovering new drugs (or novel chemical structures) very challenging. Areas covered: This review discusses triazole derivatives possessing anticancer activity (hCA inhibition) and also illustrates the recent updates on triazole moiety for hCA inhibition research emphasizing the structure activity relationship aspects. Conclusion: However, as the cellular and molecular causes of numerous diseases are better understood, more opportunities for logical therapeutic development broaden. Small molecule inhibitors of hCA IX interactions can now be found through screenings using large virtual chemical libraries and a series of novel compounds from research literature. In this context, the literature's triazole benzene sulfonamide derivatives have been thoroughly studied for structure-activity relationship and reported here for future design and development of leads.