期刊
INORGANICA CHIMICA ACTA
卷 357, 期 11, 页码 3237-3244出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.ica.2004.04.003
关键词
platinum complexes; anticancer agents; N,O-ligands; pH-sensitive cytotoxicity
Solid tumors are often hypoxic and consequently the pH in the tumoral tissue is decreasing with increasing tumor size (pH 5.5-7.4 in solid tumors versus pH 7.4 in normal tissues). This marked difference in pH value is a problem for weak base organic drugs and could advantageously be used for the introduction of pH sensitive anticancer platinum drugs. Synthesis and structure determination of (SP-4-2)-bis(2-aminoethanolato-kappa(2)N, O)platinum(II), its binding behavior to 5'-GMP and its cytotoxicity against cisplatin sensitive cell lines under standard pH screening conditions (pH 7.4) as well as in acidified cell culture medium (PH 6.0) mimicking the conditions in a number of solid tumors is presented. There is evidence that this concept in anticancer platinum therapy, namely administration of rather unreactive drugs and activation under acidic pH conditions, can be realized. (C) 2004 Elsevier B.V. All rights reserved.
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