The poor pharmacokinetics, side effects and particularly the rapid emergence of drug resistance compromise the efficiency of clinically used anticancer drugs. Therefore, the discovery of novel and effective drugs is still an extremely primary mission. Naphthalimide family is one of the highly active anticancer drug based upon effective intercalator with DNA. In this article, we review the discovery and development of 1,8‐naphthalimide moiety, and, especially, pay much attention to the structural modifications and structure activity relationships. The review demonstrates how modulation of the moiety affecting naphthalimide compound for DNA binding that is achieved to afford a profile of antitumor activity. The DNA binding of imide and ring substitution at naphthalimide, bisnaphthalimide, naphthalimide‐metal complexes is achieved by molecular recognition through intercalation mode. Thus, this synthetic/natural small molecule can act as a drug when activation or inhibition of DNA function, is required to cure or control the cancer disease. The present study is a review of the advances in 1,8‐naphthalimide‐related research, with a focus on how such derivatives are intercalated into DNA for their anticancer activities.

中文翻译：

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1,8-萘二甲酰亚胺：有效的DNA嵌入剂和癌症治疗靶标

不良的药代动力学，副作用以及特别是耐药性的迅速出现损害了临床使用的抗癌药的效率。因此，发现新颖有效的药物仍然是极为重要的任务。萘二甲酰亚胺家族是一种基于有效嵌入DNA的高活性抗癌药物之一。在本文中，我们回顾了1,8-萘二甲酰亚胺部分的发现和发展，尤其是对结构修饰和结构活性关系的关注。该综述证明了如何调节影响萘二甲酰亚胺化合物的部分以进行DNA结合以实现提供抗肿瘤活性的特征。萘二甲酰亚胺，双萘二甲酰亚胺的酰亚胺与环取代的DNA结合 萘酰亚胺金属配合物是通过嵌入模式进行分子识别而获得的。因此，当需要激活或抑制DNA功能以治愈或控制癌症时，这种合成/天然小分子可以充当药物。本研究是对1,8-萘二甲酰亚胺相关研究进展的综述，重点是这些衍生物如何插入DNA进行抗癌活性。