Herein, six ruthenium(II) terpyridine complexes, i.e. [RuCl₂(4-EtN-Phtpy)(DMSO)] (Ru1), [RuCl₂(4-MeO-Phtpy)(DMSO)] (Ru2), [RuCl₂(2-MeO-Phtpy)(DMSO)] (Ru3), [RuCl₂(3-MeO-Phtpy)(DMSO)] (Ru4), [RuCl₂(1-Bip-Phtpy)(DMSO)] (Ru5), and [RuCl₂(1-Pyr-Phtpy)(DMSO)] (Ru6) with 4′-(4-diethylaminophenyl)-2,2′:6′,2′′-terpyridine (4-EtN-Phtpy), 4′-(4-methoxyphenyl)-2,2′:6′,2′′-terpyridine (4-MeO-Phtpy), 4′-(2-methoxyphenyl)-2,2′:6′,2′′-terpyridine (2-MeO-Phtpy), 4′-(3-methoxyphenyl)-2,2′:6′,2′′-terpyridine (3-MeO-Phtpy), 4′-(1-biphenylene)-2,2′:6′,2′′-terpyridine (1-Bip-Phtpy), and 4′-(1-pyrene)-2,2′:6′,2′′-terpyridine (1-Pyr-Phtpy), respectively, were synthesized and fully characterized. The MTT assay demonstrates that the in vitro anticancer activity of Ru1 is higher than that of Ru2–Ru6 and more selective for Hep-G2 cells than for normal HL-7702 cells. In addition, various biological assays show that Ru1 and Ru6, especially the Ru1 complex, are telomerase inhibitors targeting c-myc G4 DNA and also cause apoptosis of Hep-G2 cells. With the same Ru center, the in vitro antitumor activity and cellular uptake ability of the 4-EtN-Phtpy and 1-Bip-Phtpy ligands follow the order 4-EtN-Phtpy > 1-Bip-Phtpy.

中文翻译：

---

六种高细胞毒性钌(ii)与4'-取代-2,2':6',2''-三联吡啶配合物的合成、表征和生物学评价†

这里，六种钌( II )三联吡啶络合物，即[RuCl ₂ (4-EtN-Phtpy)(DMSO)]( Ru1 )、[RuCl ₂ (4-MeO-Phtpy)(DMSO)]( Ru2 )、[RuCl ₂ (2-MeO-Phtpy)(DMSO)] ( Ru3 )、[RuCl ₂ (3-MeO-Phtpy)(DMSO)] ( Ru4 )、[RuCl ₂ (1-Bip-Phtpy)(DMSO)] ( Ru5 ) ，和 [RuCl ₂ (1-Pyr-Phtpy)(DMSO)] ( Ru6 ) 与 4'-(4-二乙氨基苯基)-2,2':6',2''-三联吡啶 (4-EtN-Phtpy)， 4'-(4-甲氧基苯基)-2,2':6',2''-三联吡啶(4-MeO-Phtpy), 4'-(2-甲氧基苯基)-2,2':6',2'' -三联吡啶 (2-MeO-Phtpy)、4′-(3-甲氧基苯基)-2,2′:6′,2′′-三联吡啶 (3-MeO-Phtpy)、4′-(1-联亚苯基)-2 ,2':6',2''-三联吡啶 (1-Bip-Phtpy) 和 4'-(1-芘)-2,2':6',2''-三联吡啶 (1-Pyr-Phtpy)分别被合成并充分表征。MTT实验表明Ru1的体外抗癌活性高于Ru2-Ru6，且对Hep-G2细胞的选择性高于对正常HL-7702细胞的选择性。此外，各种生物学测定表明，Ru1和Ru6，特别是Ru1复合物，是靶向c-myc G4 DNA的端粒酶抑制剂，也会导致Hep-G2细胞凋亡。具有相同的Ru中心，4-EtN-Phtpy和1-Bip-Phtpy配体的体外抗肿瘤活性和细胞摄取能力遵循4-EtN-Phtpy > 1-Bip-Phtpy的顺序。