Recently, we have demonstrated a unique approach to highly stereoselective asymmetric self-assembly of very stable helicate-like compounds, termed triplex metallohelices, which uniquely have unsymmetrical architectures akin to a-helical oligopeptides. Here we report the successful design and rapid synthesis of highly functionalised triplex systems which display high, structure-dependent toxicity to the human colon carcinoma cells, causing dramatic changes in the cell cycle without DNA damage. They have lower toxicity to e.g. human breast adenocarcinoma cells and normal cell lines, and perhaps most remarkably they show no significant toxicity to microbes and insect models. The mechanisms of action and origin of the selectivity will be discussed.

Functionalised peptidomimetic metallohelices

253rd National Meeting (2017)

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