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Abstract Quinoline–1,2,3‐triazole hybrids have emerged as a highly promising class of compounds in pharmaceutical chemistry due to their potent and multifaceted biological activities, particularly as anticancer and antimalarial agents. This comprehensive review highlights the exclusive pharmacological profiles of quinoline and 1,2,3‐triazole scaffolds as anticancer and antimalarial agents, along with their synthetic methodologies, strengthening their prevalence in FDA‐approved drugs and their wide‐ranging spectrum of medical applications. This review systematically examines the synergistic amalgamation of quinoline and 1,2,3‐triazole pharmacophores in a single molecular framework, leading to improved pharmacokinetic and pharmacodynamic properties, along with the structure‐activity relationship (SAR) studies emphasising the importance of specific functional group variations in increasing the potency and selectivity. This review serves as a valuable resource for researchers, summarising current progress and offering insights to guide the future design and development of quinoline‐1,2,3‐triazole hybrids as promising candidates for the treatment of cancer and malaria.
Hadavani et al. (Sat,) studied this question.