Cancer, accounts for around 10 million deaths annually, is the second leading cause of death globally. The continuous emergency of drug-resistant cancers and the low specificity of anticancer agents are the main challenges in the control and eradication of cancers, so it is imperative to develop novel anticancer agents. Immense efforts have been made in developing new lead compounds and novel chemotherapeutic strategies for the treatment of various forms of cancers in recent years. β-Lactam derivatives constitute versatile and attractive scaffolds for the drug discovery since these kinds of compounds possess a variety of pharmacological properties, and some of them exhibited promising potency against both drug-sensitive and drug-resistant cancer cell lines. Thus, β-lactam moiety is a useful template for the development of novel anticancer agents. This review will provide an overview of β-lactam derivatives with the potential therapeutic application for the treatment of cancers covering articles published between 2000 and 2020. The mechanisms of action, the critical aspects of design and structureactivity relationships are also discussed.

癌症每年导致约1000万人死亡，是全球第二大死亡原因。耐药性癌症的持续不断发展和抗癌药特异性低是控制和根除癌症的主要挑战，因此开发新型抗癌药势在必行。近年来，在开发用于治疗各种形式的癌症的新的先导化合物和新的化学治疗策略方面已经做出了巨大的努力。β-内酰胺衍生物构成了药物开发的多功能和有吸引力的支架，因为这些化合物具有多种药理特性，其中一些对药物敏感性和耐药性癌细胞系均显示出有希望的效力。因此，β-内酰胺部分是开发新型抗癌剂的有用模板。