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Organometallic Half-Sandwich Iridium Anticancer Complexes
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SYSNO ASEP 0439813 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Organometallic Half-Sandwich Iridium Anticancer Complexes Author(s) Liu, Z. (GB)
Habtemariam, A. (GB)
Pizarro, A.M. (GB)
Fletcher, S.A. (GB)
Kisová, Anna (BFU-R)
Vrána, Oldřich (BFU-R) RID
Salassa, L. (GB)
Bruijnincx, P.C.A. (GB)
Clarkson, G.J. (GB)
Brabec, Viktor (BFU-R) RID, ORCID
Sadler, P. J. (GB)Number of authors 11 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 54, č. 8 (2011), 3011-3026Number of pages 16 s. Publication form Print - P Language eng - English Country US - United States Keywords RUTHENIUM(II) ARENE COMPLEXES ; CANCER-CELL CYTOTOXICITY ; DNA-BINDING PROPERTIES Subject RIV BO - Biophysics R&D Projects GPP303/11/P047 GA ČR - Czech Science Foundation (CSF) GAP301/10/0598 GA ČR - Czech Science Foundation (CSF) UT WOS 000289697800035 DOI https://doi.org/10.1021/jm2000932 Annotation The low-spin 5d(6) Ir-III organometallic half-sandwich complexes [(eta(5)-Cp-x)Ir(XY)Cl](0/+), Cp-x = Cp*, tetramethyl(phenyl, cyclopentadienyl (Cp-xph), or tetramethyl(biphenyl)-cyclopertadienyl (Cp-xbiph), XY = 1,10-phenanthroline (4-6), 2,2'-bipyridine (7-9), ethylenediamine (10 and 11), or picolinate (12-14), hydrolyze rapidly. Complexes with N,N-chelating ligands readily form adducts with 9-ethylguanine but not 9-ethyladenine; picolinate complexes bind to both purines. Cytotoxic potency toward A2780 human ovarian cancer cells increases with phenyl substitution on Cp*: Cp-xbiph > Cp-xph > Cp*; Cp-xbiph complexes 6 and 9 have submicromolar activity. Guanine residues are preferential binding sites for 4-6 on plasmid DNA. Hydrophobicity (log P), cell and nucleus accumulation of Ir correlate with cytotoxicity, 6 > 5 > 4, they:distribute similarly within cells. The ability to displace DNA intercalator ethidium bromide from DNA correlates with cytotoxicity and viscosity of Ir DNA adducts. The hydrophobicity and intercalative ability of Cp-xph and Cp-xbiph male a major contribution to the anticancer potency of their Ir-III complexes. Workplace Institute of Biophysics Contact Jana Poláková, polakova@ibp.cz, Tel.: 541 517 244 Year of Publishing 2015
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