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

作者：Chelopo Madichaba P; Pawar Sachin A; Sokhela Mxolisi K; Govender Thavendran; Kruger Hendrik G; Maguire Glenn E M^*

来源：European Journal of Medicinal Chemistry, 2013, 66: 407-414.

DOI：10.1016/j.ejmech.2013.05.048

• Anticancer
• Tetrahydroisoquinoline
• Ruthenium

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 mu M 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.

• 出版日期2013-8