Anti-HIV and cytotoxic activities of Ru(II)/Ru(III) polypyridyl complexes containing 2,6-(2′-benzimidazolyl)-pyridine/chalcone as co-ligand

Ru(II)/Ru(III) polypyridyl complexes containing 2.6-(2'-benzimidazolyl)-pyridine or chalcone as co-ligands were synthesized and characterized proviously (Mishra, L.; Sinha, R. Indian J. Chem., Sec. A 2001, in press. Mishra. L.: Sinha, R. Indian J. Chem., Src. A, 39A, 2000, 1131). Their interaction with aqueous buffered calf thymus DNA was measured. (Novakova, O.; Kasparkova, J., Vrana, O.: van Vliet. P. M., Reedijk. J.; Brabec, V, Biochem. 34, 1995, 12369 and these results prompted additional screening for anti-HIV (human immunodeficiency virus) activity against DNA replication in H9 lymphocytes and cytotoxic activity against eight tumor cell lines. The most active compounds were 17 in the former assay (EC50 < 0.1 g/mL and TI > 23.1) and 3.8. 10, and 14 in the latter assay, especially selectively against the 1A9 ovarian cancer cell line (IC50 = 4.1, 3.8, 3.6, and 2.5 mug/mL. respectively). (C) 2001 Elsevier Science Ltd. All rights reserved.