Library of second-generation cycloruthenated compounds and evaluation of their biological properties as potential anticancer drugs: Passing the nanomolar barrier
Library of second-generation cycloruthenated compounds and evaluation of their biological properties as potential anticancer drugs: Passing the nanomolar barrier
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DOI：
10.1039/c1dt10322a
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发表时间：
2011-01-01
影响因子：
4
通讯作者：
Pfeffer, Michel
中科院分区：
文献类型：
--
作者：
Fetzer, Ludivine;Boff, Bastien;Pfeffer, Michel
合成了32个有机钌化合物库。已知和新型的C-N环金属化化合物以及这种金属的N-C-N和N-N-C钳形衍生物已被用于此目的。大多数化合物的体外抗肿瘤活性已被测试，因此已发现良好到优异的活性。一些新合成的化合物的IC50通过了纳摩尔范围的符号屏障，这表明了一个关键的改进。活性水平暂时与化合物的物理化学性质有关，如它们的Ru-III/II氧化还原电位和它们的亲脂性（log P）。
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 IC50 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).