4.6 Article

DNA interaction and antiproliferative behavior of the water soluble platinum supramolecular squares [(en)Pt(N-N)]4(NO3)8 (en = ethylenediamine, N-N-4,4′-bipyridine or 1,4-bis(4-pyridyl) tetrafluoro benzene)

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JOURNAL OF INORGANIC BIOCHEMISTRY
卷 101, 期 4, 页码 660-666

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ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2006.12.009

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supramolecular chemistry; platinum macrocycle; antitumor activity of Pt complexes; Pt complex-DNA intercalation

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The interaction with DNA of two water soluble platinum supramolecular squares [(en)Pt(N-N)](4)(NO3)(8) (en = ethylenediamine, N-N = 1,4-bis(4-pyridyl)tetrafluorobenzene, compound 1, N-N = 4,4'-bipyridine, compound 2) has been studied by circular dichroism, electrophoretic mobility and atomic force microscopy. the two complexes drastically modify the second and tertiary structures of DNA, but compound 2 does it strongly due probably to its smaller size by comparison with compound 1 and its more suitable structural features for intercalation between base pairs. The two supramolecular squares were assayed against the HL-60 tumor cell line for 24 and 72 h. The IC50 values for 24 h are smaller than that of cisplatin for this time, however for 72 h the IC50 have higher values being the corresponding to compound 2 comparable to that of cisplatin. Apoptotic assays were also carried out for the compounds 1 and 2 against the tumor cell line. (c) 2007 Elsevier Inc. All rights reserved.

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