1,8-naphthalimide-based DNA intercalators and anticancer agents: a systematic review.

IF 3.9 2区化学 Q2 CHEMISTRY, APPLIED

Molecular Diversity Pub Date : 2025-06-18 DOI:10.1007/s11030-025-11251-1

Aeyaz Ahmad Bhat, Amel Gacem, Maytham T Qasim, Nuha Almulla, Khursheed Muzammil, Manar G Shalabi

引用次数: 0

Abstract

1,8-Naphthalimide derivatives have emerged as versatile scaffolds in anticancer drug development due to their efficient DNA-intercalating ability and diverse mechanisms of action, including Topoisomerase I/II inhibition and photoinduced DNA cleavage. These structural features contribute to their potent cytotoxicity and broad-spectrum anticancer activity. This manuscript offers a focused yet comprehensive overview of recent advances in the design and biological evaluation of 1,8-naphthalimide-based intercalators. The compounds are systematically categorized into mono-intercalators, fused-ring-extended analogs, photoactive agents, bifunctional conjugates, and organometallic hybrids. For each class, we discuss structure-activity relationships, cytotoxic profiles, and mechanistic insights relevant to anticancer efficacy. Distinct from previous reviews, this work provides an integrated perspective across multiple structural classes, emphasizing their translational potential and guiding future rational design of naphthalimide-based therapeutics.

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1,8-萘酰亚胺基DNA插入剂和抗癌剂：系统综述。

1,8-萘酰亚胺衍生物由于其高效的DNA插入能力和多种作用机制，包括拓扑异构酶I/II抑制和光诱导DNA切割，已成为抗癌药物开发中的多功能支架。这些结构特征有助于其强大的细胞毒性和广谱抗癌活性。这份手稿提供了一个集中而全面的概述在设计和1,8-萘酰亚胺为基础的插入物的生物学评价的最新进展。这些化合物被系统地分类为单插入物、熔合环扩展类似物、光活性剂、双功能偶联物和有机金属杂化物。对于每节课，我们讨论结构-活性关系，细胞毒性谱，以及与抗癌功效相关的机制见解。与以往的综述不同，本研究提供了跨多个结构类的综合视角，强调了它们的转化潜力，并指导未来基于萘酰亚胺的治疗药物的合理设计。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Molecular Diversity 化学-化学综合

CiteScore

7.30

自引率

7.90%

发文量

219

审稿时长

2.7 months

期刊介绍： Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;