The current landscape of 1,2,3-triazole hybrids with anticancer therapeutic potential: Part I.

Cancer, with its steadily increasing morbidity and mortality, will continue to pose a threat to humanity over an extended period. Chemotherapeutics play an indispensable role in cancer treatment, and hundreds of drugs have been approved for this purpose. Nevertheless, the fight against cancer remains a formidable challenge. This is mainly due to the emergence of multidrug resistance and the severe side effects associated with currently available anticancer drugs. Consequently, there is an urgent imperative to explore novel chemotherapeutic agents. 1,2,3-Triazoles belong to one of the most privileged classes of nitrogen-containing five-membered heterocycles and are regarded as prominent sources for the development of innovative anticancer chemotherapeutics. 1,2,3-Triazole hybrids, which possess multitargeted mechanisms of action within the cancer progression pathway, hold the potential to overcome multidrug resistance and mitigate side effects. Furthermore, several 1,2,3-triazole hybrids have already been approved for cancer therapy or are currently under clinical evaluation. This clearly demonstrates that 1,2,3-triazole hybrids are valuable scaffolds in the treatment and eradication of cancer. This review aims to provide insights into the anticancer therapeutic potential of 1,2,3-triazole hybrids, along with their mechanisms of action, crucial aspects of design, and structure-activity relationships (SARs). It encompasses articles published from 2021 onward.