期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 102, 期 2, 页码 193-202出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2007.07.035
关键词
ruthenium complex; antitumor drug; DNA-binding; quantitative structure-activity relationship (QSAR)
A series of octahedral Ru(II) polypyridyl complexes, [Ru(phen)(2)L](2+) (L = R-PIP and PIP = 2-phenylimidazo[4,5-f][1,10]phenanthroline) were synthesized and characterized by elementary analysis, H-1 NMR and ES-MS, as well as UV-visible spectra and emission spectra. The antitumor activities of these complexes and their corresponding ligands were investigated against mouse leukemia L1210 cells, human oral epidermoid carcinoma KB cells, human promyelocytic leukemia cells (HL-60) and Bel-7402 liver cancer cells by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. It was found that the complexes [Ru(phen)(2)L](2+) (L = R-PIP) exert rather potent activities against all of these cell lines, especially for the KB cells (IC50 = 4.7 +/- 1.3 mu M). The binding affinities of these Ru(II) complexes to CT-DNA (calf thymus DNA), as well as the DNA-unwinding properties on supercoiled pBR322 DNA were also investigated. The results showed that these Ru(II) polypyridyl complexes not only had an excellent DNA-binding property but also possessed a highly effective DNA-photocleavage ability. The structure-activity relationships and antitumor mechanism were also carefully discussed. (c) 2007 Elsevier Inc. All rights reserved.
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