In the present study, the synthesis of three 1,8-naphthalimide-acridinyl hybrids (2a, 2b, and 5b) using N-amido-1,8-naphthalimides (1 and 4) and acridinyl isothiocyanates is reported. The newly synthesized hybrids were evaluated for their anticancer activity in six human cancer cell lines (HL-60, MT-4, HepG2, HeLa, SK-OV-3, and MCF-7). Their inhibition activity against DNA-topoisomerase I (Topo I) and Electrophorus electricus acetylcholinesterase (AChE) was also studied. The results indicate that 2b displayed good cytotoxicity for MT-4, HepG2, HeLa, and SK-OV-3 with the IC50 values of 14.66 ± 0.31, 27.32 ± 2.67, 17.51 ± 0.34, and 32.26 ± 1.74 μM, respectively. All compounds, especially 2b, exhibited obvious bands corresponding to DNA fragments at 0.5 mM concentration, further confirming the pharmacological mechanism related to the Topo I inhibitory activities. In addition, compound 2a exhibited higher inhibition activity against AChE than 2b and 5b, with IC50 values of 0.32 ± 0.04 mM, and the acridinyl ring may contribute to the activity of 2a.

中文翻译：

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一些1,8-萘二甲酰亚胺-吖啶杂化物的合成与生物学评价

在本研究中，报道了使用 N-amido-1,8-naphthalimides（1 和 4）和吖啶基异硫氰酸酯合成三个 1,8-naphthalimide-吖啶杂化物（2a、2b 和 5b）。在六种人类癌细胞系（HL-60、MT-4、HepG2、HeLa、SK-OV-3 和 MCF-7）中评估了新合成的杂交体的抗癌活性。还研究了它们对 DNA 拓扑异构酶 I (Topo I) 和电泳乙酰胆碱酯酶 (AChE) 的抑制活性。结果表明2b对MT-4、HepG2、HeLa和SK-OV-3表现出良好的细胞毒性，IC50值分别为14.66±0.31、27.32±2.67、17.51±0.34和32.26±1.74μM 所有化合物，尤其是 2b，在 0.5 mM 浓度下显示出与 DNA 片段相对应的明显条带，进一步证实了与 Topo I 抑制活性相关的药理机制。此外，化合物2a对AChE的抑制活性高于2b和5b，IC50值为0.32±0.04 mM，并且吖啶环可能有助于2a的活性。