| Literature DB >> 18755512 |
Michael R Reithofer1, Anne Schwarzinger, Seied M Valiahdi, Markus Galanski, Michael A Jakupec, Bernhard K Keppler.
Abstract
(OC-6-33)-Dichlorido(ethane-1,2-diamine)dihydroxidoplatinum(IV) (1) was carboxylated using succinic- or 3-methylglutaric anhydride. The resulting bis(carboxylato)platinum(IV) complexes display free, uncoordinated carboxylic acid groups which were further derivatized with primary aliphatic alcohols. The complexes were characterized in detail by elemental analysis, ESI-MS, FT-IR, as well as multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy. Cytotoxic properties were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1, SK-OV-3), cervical carcinoma (HeLa) and colon carcinoma (SW480) by means of the MTT assay (MTT = 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide). Structure-activity relationships showed that the cytotoxicity increased with increasing lipophilicity of the alcoholate moiety yielding IC50 values in the low micromolar or even low nanomolar range.Entities:
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Year: 2008 PMID： 18755512 DOI： 10.1016/j.jinorgbio.2008.07.006
Source DB: PubMed Journal: J Inorg Biochem ISSN： 0162-0134 Impact factor: 4.155