Department of Oncology, Zhuji Affiliated Hospital of Shaoxing University, Zhejiang Province 311800, China.
Chongqing Institute of Engineering, Chongqing 400056, China.
Curr Top Med Chem. 2020;20(16):1468-1480. doi: 10.2174/1568026620666200309161444.
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.
癌症每年导致约 1000 万人死亡，是全球第二大死亡原因。耐药性癌症的不断出现和抗癌药物的低特异性是癌症控制和根除的主要挑战，因此开发新型抗癌药物迫在眉睫。近年来，人们为开发治疗各种形式癌症的新先导化合物和新化疗策略做出了巨大努力。β-内酰胺衍生物是药物发现的多功能和有吸引力的支架，因为这些化合物具有多种药理特性，其中一些对敏感和耐药癌细胞系表现出有希望的活性。因此，β-内酰胺部分是开发新型抗癌药物的有用模板。本文综述了 2000 年至 2020 年间发表的具有治疗癌症应用潜力的β-内酰胺衍生物，讨论了它们的作用机制、设计的关键方面和构效关系。
