Abstract
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.
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