Influence of Hydrogen-Bonding Substituents on the Cytotoxicity of RAPTA Compounds

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• 作者：Claudine Scolaro ; Tilmann J. Geldbach ; Sé ; bastien Rochat ; Antoine Dorcier ; Christian Gossens ; Alberta Bergamo ; Moreno Cocchietto ; Ivano Tavernelli ; Gianni Sava ; Ursula Rothlisberger ; and Paul J.
• 刊名：Organometallics
• 出版年：2006
• 出版时间：January 30, 2006
• 年：2006
• 卷：25
• 期：3
• 页码：756 - 765
• 全文大小：390K
• 年卷期：v.25,no.3(January 30, 2006)
• ISSN：1520-6041

文摘

A new series of organometallic ruthenium(II)-arene compounds of the type RuCl₂(mages/gifchars/eta.gif" BORDER=0 >⁶-arene)(phosphine)(phosphine = 1,3,5-triaza-7-phosphaadamantane, PTA, and 3,7-diacetly-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane, DAPTA) with different potential hydrogen-bonding functionalities on the arene ligandhave been prepared and studied for their antitumor activity. Cell viability studies using the TS/A mouseadenocarcinoma cancer cell line and the nontumorigenic HBL-100 human mammary cell line, combinedwith uptake determinations, are compared to the nonfunctionalized analogues, previously shown to beactive on solid metastasizing tumors. The reactivity of the functionalized RAPTA compounds with a14-mer oligonucleotide (established by mass spectrometry) has been rationalized by DFT calculations,which indicate that environmental factors are important.