Anticancer activity of ruthenium(II) arene complexes bearing 1,2,3,4-tetrahydroisoquinoline amino alcohol ligands

• First TIQ amino alcohol based Ru complexes.
• Excellent selectivity index.
• First comparison of the anti cancer activity for the diastereomers TIQ compounds.

Ruthenium complexes offer potential reduced toxicity compared to current platinum anticancer drugs. 1,2,3,4-tetrahydrisoquinoline amino alcohol ligands were synthesised, characterised and coordinated to an organometallic Ru(II) centre. These complexes were evaluated for activity against the cancer cell lines MCF-7, A549 and MDA-MB-231 as well as for toxicity in the normal cell line MDBK. They were observed to be moderately active against only the MCF-7 cells with the best IC50 value of 34 μM for the cis-diastereomeric complex C4. They also displayed excellent selectivity by being relatively inactive against the normal MDBK cell line with SI values ranging from 2.3 to 7.4.

The facile synthesis of the ruthenium complexes of 1,2,3,4-tetrahydrisoquinoline amino alcohol ligands is described. These complexes demonstrated excellent toxicity selectivity between the MCF-7 cancer cell line and the MDBK healthy cell line.Figure optionsDownload as PowerPoint slide