NDLI: Anticancer activity of heteroleptic diimine complexes of dirhodium: A study of intercalating properties, hydrophobicity and <i>in cellulo</i> activity

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Anticancer activity of heteroleptic diimine complexes of dirhodium: A study of intercalating properties, hydrophobicity and in cellulo activity

Content Provider	Royal Society of Chemistry (RSC)
Author	Aguirre, J. Dafhne Chouai, Abdellatif Angeles-Boza, Alfredo M. Turro, Claudia Pellois, Jean-Philippe Dunbar, Kim R.
Copyright Year	2009
Abstract	The series of complexes cis-[Rh2(μ-O2CCH3)2(dppn)(L)]2+, where dppn = benzo[i]dipyrido[3,2-a:2′,3′-c] phenazine, and L = bpy (2,2′-bipyridine) (1), phen (1,10-phenanthroline) (2), dpq (dipyrido[3,2-f:2′,3′-h]quinoxaline) (3), dppz (dipyrido[3,2-a:2′,3′-c]phenazine) (4), and dppn (5) were synthesized and their effect on the human cancer cells HeLa and COLO-316 was monitored. Complexes 1 and 2 interact with DNA through intercalation, whereas compounds 3–5 bind only electrostatically. It was found that the dirhodium complex 4 is the most effective compound at inhibiting cell viability of the human cancer cells HeLa and COLO-316. A general conclusion is that the hydrophobicity of the compounds correlates with their in cellulo activity in both cell lines. The ability of the compounds to reach nuclear DNA and form adducts was explored using the comet assay. The results indicate that compounds 1–5 either do not form adducts with DNA that are detrimental to the cell or that they are successfully repaired by the cellular machinery. The results of an annexin V assay indicate that compounds 1–4 trigger apoptosis, whereas compound 5 clearly does not. These findings are significant because they support the contention that dirhodium complexes can be tuned to direct their effect to cellular targets other than nuclear DNA.
Starting Page	10806
Ending Page	10812
Page Count	7
File Format	HTM / HTML PDF
ISSN	14779226
Volume Number	0
Issue Number	48
Journal	Dalton Transactions
DOI	10.1039/b915357h
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	Phenazine Bipyridine Phenanthroline Quinoxaline Cancer HeLa Interaction DNA Hydrophobe Comet assay Annexin A5 Apoptosis
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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