van Zutphen Steven, Pantoja Elena, Soriano Rosario, Soro Carlos, Tooke Duncan M, Spek Anthony L, den Dulk Hans, Brouwer Jaap, Reedijk Jan
Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, P.O. Box 9502, 2300, RA Leiden, The Netherlands.
Dalton Trans. 2006 Feb 28(8):1020-3. doi: 10.1039/b512357g. Epub 2005 Dec 7.
New asymmetric trans-platinum(II) complexes, composed of an isopropylamine, an azole and two carboxylate leaving groups, are presented. The crystal and molecular structures of one of the complexes has been determined and the cytotoxicity and reactivity with 5'-guanosine monophosphate is reported. The complexes show a reduced reactivity, but no decrease in cytotoxic activity compared to their chloro-counterparts. Furthermore the complexes largely overcome cisplatin resistance, they therefore present an interesting class of antitumour active trans-platinum complexes.
本文介绍了由异丙胺、唑和两个羧酸离去基团组成的新型不对称反式铂（II）配合物。已确定其中一种配合物的晶体和分子结构，并报道了其细胞毒性以及与5'-鸟苷单磷酸的反应活性。与它们的氯取代类似物相比，这些配合物的反应活性降低，但细胞毒性活性并未降低。此外，这些配合物在很大程度上克服了顺铂耐药性，因此它们是一类有趣的具有抗肿瘤活性的反式铂配合物。
