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萘酰亚胺衍生物作为抗癌剂的构效关系(SAR)展望。

An Outlook of the Structure Activity Relationship (SAR) of Naphthalimide Derivatives as Anticancer Agents.

机构信息

Department of Chemistry, School of Physical Sciences, Lovely Professional University, Phagwara, 144411, India.

出版信息

Anticancer Agents Med Chem. 2024;24(2):96-116. doi: 10.2174/0118715206274007231107094411.

Abstract

The efficacy of drugs against cancer in clinical settings may be limited due to pharmacokinetic issues, side effects and the emergence of drug resistance. However, a class of anticancer drugs known as naphthalimides have proven to be very effective. These derivatives have demonstrated to be effective in treating different types of cancers and exhibit strong DNA binding affinity. The anticancer properties of the naphthalimide derivatives allow them to target a number of cancer cell lines. Researchers have investigated the anticancer activity of numerous naphthalimide derivatives, such as heterocyclic fused, non-fused substituted, metal-substituted and carboxamide derivatives. Surprisingly, some derivatives demonstrate greater activity than the reference norms, such as cisplatin, amonafide, mitonafide and others and are selective against many cell lines. The primary objective of this research is to comprehend the effects of various substitution patterns on the structure-activity relationship (SAR) of these derivatives and the instances in which they enhance or reduce this biological activity.

摘要

由于药代动力学问题、副作用和耐药性的出现,癌症在临床治疗中的药物疗效可能会受到限制。然而,一类被称为萘酰亚胺的抗癌药物已被证明非常有效。这些衍生物已被证明在治疗不同类型的癌症方面非常有效,并表现出很强的 DNA 结合亲和力。萘酰亚胺衍生物的抗癌特性使它们能够针对许多癌细胞系。研究人员已经研究了许多萘酰亚胺衍生物的抗癌活性,例如杂环融合、非融合取代、金属取代和羧酰胺衍生物。令人惊讶的是,一些衍生物比顺铂、阿莫奈非、米托奈非等参考标准具有更高的活性,并且对许多细胞系具有选择性。本研究的主要目的是了解各种取代模式对这些衍生物的结构-活性关系(SAR)的影响,以及它们增强或降低这种生物活性的情况。

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