Cancer, accounts for around 10 million deaths annually, is the second leading cause of death globally. The 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’s 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 interesting scaffolds for the drug discovery since this kind 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 potential therapeutic application for treatment of cancers covering articles published between 2000 and 2020. The mechanisms of action, the critical aspects of design and structure-activity relationships are also discussed.
Keywords: hybrid compounds, anticancer, drug-resistant, structure-activity relationship, βlactam
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