School of Chemical Engineering and Physical Sciences, Lovely Professional University, Phagwara 144411, India.
School of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala 147004, India.
Bioorg Chem. 2022 Apr;121:105677. doi: 10.1016/j.bioorg.2022.105677. Epub 2022 Feb 12.
1,8-Naphthalimide moiety is well known to possess various biological activities as it can very well intercalate with DNA. In recent years, much of the attention has been given to the preparation of naphthalimide derivatives by substitution at various positions of the 1,8-naphthalimide ring for their exploration as anticancer agents. These derivatives possess different anticancer properties, which cover a broader range of cancer cell lines. Interestingly, some derivatives include enhanced activity than the reference standards like cisplatin, amonafide, mitonafide, etc., and be selective against the cell lines. The aim is to study the effect of different modulations at various positions of the 1,8-naphthalimide ring with a polyamine, thiourea, benzothiazole, benzimidazole, and formation of metal complexes and bis-naphthalimides that affects the overall cytotoxic properties of the resulting 1,8-naphthalimides. Moreover, the structure-activity relationship of these variations for the resulting derivatives' anticancer properties has also been discussed. Thus, this review will be important for a wide range of researchers to design and development of various 1,8-naphthalimide derivatives with desired drug profiles.
1,8-萘酰亚胺部分由于其与 DNA 很好地进行嵌入作用而具有多种生物活性,因此备受关注。近年来,人们对萘酰亚胺衍生物的制备给予了极大的关注,通过在萘酰亚胺环的各个位置进行取代,探索其作为抗癌药物的应用。这些衍生物具有不同的抗癌特性,涵盖了更广泛的癌细胞系。有趣的是,一些衍生物的活性比顺铂、氨莫氟、米托蒽醌等参考标准更高,并且对细胞系具有选择性。本研究旨在研究不同取代基在 1,8-萘酰亚胺环的不同位置对多胺、硫脲、苯并噻唑、苯并咪唑的影响,并形成金属配合物和双萘酰亚胺,从而影响所得 1,8-萘酰亚胺的整体细胞毒性。此外,还讨论了这些变化对所得衍生物抗癌性能的构效关系。因此,本综述对于广泛的研究人员来说非常重要,有助于设计和开发具有所需药物特性的各种 1,8-萘酰亚胺衍生物。