Cholic acid–carboplatin compounds (CarboChAPt) as models for specific drug delivery: synthesis of novel carboplatin analogous derivatives and comparison of the cytotoxic properties with correspo

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• 作者：Paschke ; Reinhard ; Kalbitz ; Jutta ; Paetz ; Christian ; Luckner ; Martin ; Mueller ; Thomas ; Schmoll ; Hans-Joachim ; et. al.
• 关键词：Alkyl spacer ; Antitumor activity ; Bile acid ; Carboplatin ; Cytostatic activity ; Platinum complexes
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2003
• 出版时间：April 1, 2003
• 年：2003
• 卷：94
• 期：4
• 页码：335-342
• 全文大小：643 K

文摘

This report continues our work on new compounds which consist of three functional parts—a transport fragment, a spacer and a biologically active ‘drug’ component. Here cholic acid functions as the transport fragment, linked via an alkyl spacer to a carboplatin analog, representing the drug (carbo-ChAPt—Fig. 1). We describe the synthesis and characterization of the series of complexes [Pt(Cyclobutane-1,1-dicarboxylato)(diamine)], {diamine=CholCOO(CH₂)_nCH(CH₂NH₂)₂ and THP(CH₂)_nCH–(CH₂NH₂)₂, n