8-Hydroxyquinolines (HQ), including clioquinol, possess cytotoxic properties and are widely used as ligands for metal-based anticancer drug research. The number and identity of substituents on the HQ can have a profound effect on activity for a variety of inorganic compounds. Ruthenium complexes of HQ exhibit radically improved potencies, and operate by a new, currently unknown, mechanism of action. To define structure-activity relationships (SAR), a family of 22 Ru(II) coordination complexes containing mono-, di- and tri-substituted hydroxyquinoline ligands were synthesized and their biological activity evaluated. The complexes exhibited promising cytotoxic activity against a cancer cell line, and the SAR data revealed the 2- and 7-positions as key sites for the incorporation of halogens to improve potency. The Ru(II) complexes potently inhibited translation, as demonstrated by an in-cell translation assay. The effects were seen at 2–15-fold higher concentrations than those required to observe cytotoxicity, suggesting that prevention of protein synthesis may be a primary, but not the exclusive mechanism for the observed cytotoxic activity.

8-羟基喹啉（HQ），包括氯喹醇，具有细胞毒性，被广泛用作金属基抗癌药物研究的配体。HQ上取代基的数量和特性可能对多种无机化合物的活性产生深远影响。总部的钌络合物显示出显着改善的效能，并通过一种新的，目前未知的作用机理起作用。为了定义结构-活性关系（SAR），合成了包含单，双和三取代的羟基喹啉配体的22 Ru（II）配位化合物家族，并对其生物学活性进行了评估。该复合物对癌细胞系表现出有希望的细胞毒性活性，SAR数据显示2位和7位是掺入卤素以提高效力的关键位点。如细胞内翻译测定所证实，Ru（II）复合物有效抑制翻译。所观察到的效果比观察细胞毒性所需浓度高2-15倍，表明预防蛋白质合成可能是观察到的细胞毒性活性的主要机制，但不是排他性机制。