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

被引：60

作者：

Chelopo, Madichaba P. ^{[1
]}

Pawar, Sachin A. ^{[1
]}

Sokhela, Mxolisi K. ^{[1
]}

Govender, Thavendran ^{[1
]}

Kruger, Hendrik G. ^{[1
]}

Maguire, Glenn E. M. ^{[1
]}

机构：

[1] Univ KwaZulu Natal, Sch Hlth Sci, Catalysis & Peptide Res Unit, ZA-4000 Durban, KwaZulu Natal, South Africa

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 66卷

基金：

新加坡国家研究基金会;

关键词：

Anticancer; Tetrahydroisoquinoline; Ruthenium; CYTOTOXIC ACTIVITY; ANTITUMOR-ACTIVITY; BREAST-CANCER; CELL-LINES; TETRAHYDROISOQUINOLINES; DERIVATIVES; CHEMISTRY; MEDICINE; BIOLOGY; ACIDS;

D O I：

10.1016/j.ejmech.2013.05.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：407 / 414

页数：8

共 49 条

[1] In vitro and in vivo activity and cross resistance profiles of novel ruthenium (II) organometallic arene complexes in human ovarian cancer [J].