Abstract
Two novel mixed-ligand ruthenium(II) complexes cis-[RuClL(PP)2]+ and cis-[RuL2(PP)2]2+ (L=1,6-diaminohexane (1,6-dahx), 1-aminohexane (1-ahx); PP=2,2′-bipyridine (bpy), 1,10-phenanthroline (phen), 4,7-diphenyl-1,10-phenanthroline (Ph2phen)) were synthesized and characterized. The apparent DNA-binding constants (Kapp) of cis-[RuCl(1,6-dahx)(bpy)2]+ (1) and cis-[Ru(1,6-dahx)2(bpy)2]2+ (3) for H-bonding to DNA were larger than those of cis-[RuCl(1,6-ahx)(bpy)2]+ (2) and cis-[Ru(1,6-ahx)2(bpy)2]2+ (4) with no H-bonding. Furthermore, the Kapp value of 3 was larger than that of 1 possessing two binding modes: covalent bonding and H-bonding with DNA. The Kapp values of cis-[RuCl(1,6-dahx)(phen)2]+ (5) and cis-[Ru(1,6-dahx)2(phen)2]2+ (6) with partial intercalation in DNA were 3–5 times larger than those of 1 and 3. Although the chemical nuclease activity of 1–6 was observed in the presence of H2O2, these complexes showed no cytotoxic activity against HeLa and cisplatin-sensitive L1210 cell lines because of the negative log Po/w values. However, it is noteworthy that 1–4 were 1.5–17 times more active than cisplatin in the cisplatin-resistant L1210/cisR cell line. cis-[RuCl(1-dahx)(Ph2phen)2]+ (7) and cis-[Ru(1-dahx)2(Ph2phen)2]2+ (8) had the positive log Po/w values with favorable cytotoxic activity against the HeLa cell line and inhibited the activity of both Topo I and II.
Published Version
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