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).
A library of 29 organoosmium compounds has been built up with known and novel cyclometalated compounds obtained with C-N, N(∧)C(∧)N, and C(∧)N(∧)N ligands. All compounds have been tested for their in vitro cytotoxic properties against A172, a tumor cell line derived from a human glioblastoma, this affording a contrasted picture of the activities of the compounds gathered in this study. Some compounds displayed good to excellent activities, some of them showing IC50 in the nanomolar range. The level of activity was tentatively correlated to several physicochemical properties of the compounds such as their E(0)1/2(Os(III/II)) redox potential and their lipophilicity (log Po/w). A parallel with related ruthenium derivatives was tentatively proposed.
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