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 previously (Mishra, L.; Sinha, R. Indian J. Chem., Sec. A 2001, in press. Mishra, L.; Sinha, R. Indian J. Chem., Sec. 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 (EC(50) < 0.1 microg/mL and TI > 23.1) and 3, 8, 10, and 14 in the latter assay, especially selectively against the 1A9 ovarian cancer cell line (IC(50) = 4.1, 3.8, 3.6, and 2.5 microg/mL, respectively).
Mishra
L
L
Department of Chemistry, Banaras Hindu University, India. khlee@email.unc.edu
Sinha
R
R
Itokawa
H
H
Bastow
K F
KF
Tachibana
Y
Y
Nakanishi
Y
Y
Kilgore
N
N
Lee
K H
KH
D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002599:Chalcone / Q000737:chemistry*; D004261:DNA Replication / Q000187:drug effects; D004279:DNA, Viral / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008024:Ligands; D010051:Ovarian Neoplasms / Q000473:pathology; D011725:Pyridines / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D004279:DNA, Viral; D008024:Ligands; D011725:Pyridines; D002599:Chalcone; D012428:Ruthenium