制备、表征并测试了含有三苯基膦二酰胺配体的钌配合物对各种癌细胞系和疟原虫恶性疟原虫的生物活性。使用 MTT 测定研究 M（单取代）和 B（双取代）复合物对人宫颈癌 (HeLa) 细胞系的影响。 24 种合成的钌配合物中的 5 种（B2、B3、B5、B6 和 B13）表现出显着的效果，IC50 值范围在 0.3 至 2.3 μM 之间。通过荧光光谱法对 B2 和 B13 的潜在生物分子靶标进行评估，揭示了与 BSA 的相关相互作用，并且与 ctDNA 的亲和力较弱。选择复合物 M2、B2、M13 和 B13 进行进一步的生物学表征。将它们对两种卵巢癌细胞系活力的影响与正常细胞系进行比较，表明它们的选择性。在治疗四种不同的耐药妇科癌细胞系（其多重耐药表型不同）时，双取代复合物的功效比单取代对应物更强。与不太敏感的 MDR 细胞相比，非 MDR 细胞对所有测试的复合物都敏感。在对复合物 M2、M13、B2 和 B13 对恶性疟原虫敏感和多重耐药寄生虫菌株的研究中，双取代复合物再次被证明是最有效的，对两种菌株均具有亚微摩尔活性。此外，复合物的耐药指数大约等于 1，比二磷酸氯喹低至少 5 倍，表明这些复合物能够在寄生虫的耐药形式中保留其活性。版权所有 © 2024。由 Elsevier 出版公司

Ruthenium complexes containing triphenylphosphine diamide ligands were prepared, characterized, and tested for their biological activity against various cancer cell lines and the malaria parasite, Plasmodium falciparum. The effect of M (mono-substituted) and B (bis-substituted) complexes on the human cervical carcinoma (HeLa) cell line was investigated using the MTT assay. Five (B2, B3, B5, B6, and B13) of the 24 synthesized ruthenium complexes showed significant effects with IC50 values ranging between 0.3 and 2.3 μM. Evaluation of the potential biomolecular targets of B2 and B13 by fluorescence spectroscopy revealed relevant interactions with BSA and only a weak affinity for ctDNA. Complexes M2, B2, M13 and B13 were selected for further biological characterization. Their effect on the viability of two ovarian cancer cell lines was compared to normal cell lines, denoting their selectivity. Upon treatment of four different drug-resistant gynaecological cancer cell lines, differing in their multidrug-resistant phenotypes, the efficacy of the bis-substituted complexes was shown to be greater than their mono-substituted counterparts. The non-MDR cells are sensitive to all the tested complexes, compared to MDR cells which are less sensitive. Upon investigation of complexes M2, M13, B2, and B13 against sensitive and multidrug-resistant parasite strains of P. falciparum, the bis-substituted complexes were again shown to be the most potent, with submicromolar activity against both strains. Furthermore, the resistance indexes for the complexes were approximately equal to 1, which is at least 5-fold lower than chloroquine diphosphate, suggesting the ability of these complexes to retain their activity in resistant forms of the parasite.Copyright © 2024. Published by Elsevier Inc.