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

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• 作者：Madichaba P. Chelopo ; Sachin A. Pawar ; Mxolisi K. Sokhela ; Thavendran Govender ; Hendrik G. Kruger ; Glenn E.M. Maguire
• 关键词：Anticancer ; Tetrahydroisoquinoline ; Ruthenium
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：August, 2013
• 年：2013
• 卷：66
• 期：Complete
• 页码：407-414
• 全文大小：438 K

文摘

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?¦ÌM 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.