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第二代环钌化合物库的构建及其作为潜在抗癌药物的生物学特性评价:突破纳摩尔级障碍。

Library of second-generation cycloruthenated compounds and evaluation of their biological properties as potential anticancer drugs: passing the nanomolar barrier.

机构信息

Institut de Chimie, UMR 7177, CNRS, Université de Strasbourg, 4, rue Blaise Pascal, 67000, Strasbourg, France.

出版信息

Dalton Trans. 2011 Sep 21;40(35):8869-78. doi: 10.1039/c1dt10322a. Epub 2011 Aug 12.

DOI:10.1039/c1dt10322a
PMID:21837342
Abstract

A library of 32 organoruthenium compounds has been synthesised. Known and novel C-N cyclometalated compounds as well as N-C-N and N-N-C pincer derivatives of this metal have been used in this purpose. Most of the compounds have been tested for their in vitro antitumoral behaviours, good to excellent activities have thus been found. Several of the newly synthesized compounds pass the symbolic barrier of the nanomolar range for their IC(50) indicating a critical improvement. The level of activity is tentatively correlated to physicochemical properties of the compounds such as their Ru(III/II) redox potential and their lipophilicity (log P).

摘要

已经合成了 32 种有机钌化合物库。为此目的,使用了已知和新型的 C-N 环金属化化合物以及该金属的 N-C-N 和 N-N-C 夹式衍生物。大多数化合物都经过了体外抗肿瘤活性测试,发现具有良好到优异的活性。新合成的几种化合物的 IC(50) 值达到了纳米级,表明有了显著的提高,从而越过了象征性的界限。活性水平与化合物的物理化学性质(如 Ru(III/II) 氧化还原电位和疏水性(log P))之间存在着暂时的相关性。

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