β-Lactam, commonly referred as azetidin-2-one, is a multifunctional building block for synthesizing β-amino ketones, γ-amino alcohols, and other compounds. Besides its well known antibiotic activity, this ring system exhibits a wide range of activities, attracting the attention of researchers. However, the structurally diverse β-lactam analogues as anticancer agents and their different molecular targets are poorly discussed. The purpose of this review is 3-fold: (1) to explore the molecular hybridization approach to design β-lactams hybrids as anticancer agents; (2) the structure activity relationship of the most active anticancer β-lactams and (3) to summarize their antitumor mechanisms.

β-内酰胺，通常称为azetidin-2-one，是用于合成β-氨基酮，γ-氨基醇和其他化合物的多功能构件。除了其众所周知的抗生素活性外，该环系统还具有广泛的活性，吸引了研究人员的注意。然而，关于结构多样的β-内酰胺类似物作为抗癌剂及其分子靶标的讨论很少。这篇综述的目的是三方面的：（1）探索分子杂交方法来设计β-内酰胺类杂种作为抗癌剂；（2）最活跃的抗癌β-内酰胺的结构活性关系和（3）总结其抗肿瘤机制。