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Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes
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Bugarcic, Tijana, Novakova, Olga, Halamikova, Anna, Zerzankova, Lenka, Vrana, Oldrich, Kasparkova, Jana, Habtemariam, Abraha, Parsons, S. (Simon), Sadler, P. J. and Brabec, V. (Viktor). (2008) Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes. Journal of Medicinal Chemistry, Vol.51 (No.17). pp. 5310-5319. ISSN 0022-2623
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Official URL: http://dx.doi.org/10.1021/jm8003043
Abstract
We have compared the cancer cell cytotoxicity, cell uptake., and DNA binding properties of the isomeric terphenyl complexes [(eta(6)-arene)Ru(en)Cl](+), where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, or p-terp). Complex 1, the X-ray crystal structure of which confirms that it has the classical "piano-stool" geometry, has a similar potency to cisplatin but is not cross-resistant and has a much higher activity than 2 or 3. The extent of Ru uptake into A2780 or A2780cis cells does not correlate with potency. Complex I binds to DNA rapidly and quantitatively, preferentially to guanine residues, and causes significant DNA unwinding. Circular and linear dichroism, competitive binding experiments with ethidium bromide, DNA melting, and surface-enhanced Raman spectroscopic data are consistent with combined intercalative and monofunctional (coordination) binding mode of complex 1. This unusual DNA binding mode may therefore make a major contribution to the high potency of complex 1.
| Item Type: | Journal Article |
|---|---|
| Subjects: | Q Science > QD Chemistry Q Science > QP Physiology |
| Divisions: | Faculty of Science > Chemistry |
| Library of Congress Subject Headings (LCSH): | Cell-mediated cytotoxicity, DNA-binding proteins, Ruthenium compounds, DNA-drug interactions |
| Journal or Publication Title: | Journal of Medicinal Chemistry |
| Publisher: | American Chemical Society |
| ISSN: | 0022-2623 |
| Date: | 11 September 2008 |
| Volume: | Vol.51 |
| Number: | No.17 |
| Number of Pages: | 10 |
| Page Range: | pp. 5310-5319 |
| Identification Number: | 10.1021/jm8003043 |
| Status: | Peer Reviewed |
| Publication Status: | Published |
| Access rights to Published version: | Restricted or Subscription Access |
| Funder: | Czech Republic. Ministerstvo školství, mládeže a tělovýchovy [Czech Republic. Ministry of Education, Youth, and Sport], Akademie věd České republiky [Academy of Sciences of the Czech Republic] (ASCR), Ministerstvo zdravotnictví České republiky [Ministry of Health of the Czech Republic] (MZCR) |
| Grant number: | MSMT LC06030 (CRMEYS), 6198959216 (CRMEYS), ME08017 (CRMEYS), OC08003 (CRMEYS), 1QS500040581 (ASCR), KAN200200651 (ASCR), AV0Z50040507 (ASCR), AV0Z50040702 (ASCR), IAA400040803 (ASCR), NR8562-4/2005 (MZCR) |
| URI: | http://wrap.warwick.ac.uk/id/eprint/29419 |
Data sourced from Thomson Reuters' Web of Knowledge
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