期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 100, 期 10, 页码 1579-1585出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2006.05.001
关键词
cisplatin analogues; pyrazole ligands; DNA lesions; DNA modifications
In search for new platinum-based anticancer drugs, four cisplatin analogues, which contain pyrazole rings as non-leaving ligands, have been synthesized: CiS-PtCl2(3,5-DM HMPz)(2), CiS-PtCl2(Pz)(2), CiS-PtCl2(CIMPz)(2), and CiS-PtCl2(HMPz)(2), where Pz = pyrazole, H = hydroxyl, M = methyl. We tested their cytotoxicity, apoptosis induction ability, DNA damaging and modification properties comparing them in respect to the parent compound. The cytotoxic activity of these platinum pyrazole complexes toward the murine leukemia cell line was 2.9-3.8 times lower than actvity of cisplatin. The tested compounds varied in their mechanism of action by producing different DNA lesions. The most interesting compound seems to be the complex with chloromethyl groups at NI of pyrazole rings, which exhibited the highest ability to form bifunctional adducts with DNA in vitro. (c) 2006 Elsevier Inc. All rights reserved.
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