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.
Keywords: β-lactam, Hybrid compounds, Anticancer, Drug-resistant, Structure-activity relationship, Cancer cell lines.
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