Chemotherapy is an important therapeutic approach for the treatment of cancer. Currently, many anticancer drugs are available in the market that plays an important role in cancer treatment, but concerns such as, drug resistance and side effects create an urgent need for the development of new anti-tumor drugs with high potency and less side effects. Heterocycles are of great interest due to their fascinating anticancer activity. Among them, 1,3,4-oxadiazoles showed attracting anti-tumor activity and its derivatives are under clinical trials for the treatment of cancer. Hybridization of 1,3,4-oxadiazole moiety with other heterocyclic pharmacophoresis a promising approach to overcome various disadvantages of current anticancer drugs such as drug resistance, toxicity, and other side effects. Thus, 1,3,4-oxadiazole-heterocycle hybrids occupy a significant position in the discovery of anti-tumor drugs. Among the reported oxadiazole-based hybrids reviewed here, compounds 45i, 59j, and 62x showed the highest anticancer activity with IC₅₀ values in the nanomolar range. This review summarizes the recent developments in the anticancer potential, structure–activity relationships, and mechanisms of actions of 1,3,4-oxadiazole-heterocycle hybrids.

化疗是治疗癌症的重要治疗方法。目前，市场上有许多抗癌药物在癌症治疗中发挥着重要作用，但由于耐药性和副作用等问题，迫切需要开发高效、副作用小的新型抗肿瘤药物。杂环化合物因其迷人的抗癌活性而备受关注。其中，1,3,4-恶二唑显示出吸引抗肿瘤活性，其衍生物正在临床试验中用于治疗癌症。1,3,4-恶二唑部分与其他杂环药效团的杂交是克服当前抗癌药物的各种缺点（例如耐药性、毒性和其他副作用）的有前途的方法。因此，1,3，4-恶二唑-杂环化合物在抗肿瘤药物的发现中占有重要地位。在此处审查的报告的基于恶二唑的杂化物中，化合物45i、59j和62x显示出最高的抗癌活性，IC ₅₀值在纳摩尔范围内。本综述总结了 1,3,4-恶二唑-杂环化合物的抗癌潜力、构效关系和作用机制的最新进展。