Abstract

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.

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