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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Pyrithione-based ruthenium complexes as inhibitors of aldo-keto reductase 1C enzymes and anticancer agents
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Pyrithione-based ruthenium complexes as inhibitors of aldo-keto reductase 1C enzymes and anticancer agents

机译：基于吡啶酮的钌配合物作为醛酮还原酶1C酶和抗癌剂的抑制剂

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摘要

Four ruthenium complexes of clinically used zinc ionophore pyrithione and its oxygen analog 2-hydroxy-pyridine N-oxide were prepared and evaluated as inhibitors of enzymes of the aldo-keto reductase subfamily 1C (AKR1C). A kinetic study assisted with docking simulations showed a mixed type of inhibition consisting of a fast reversible and a slow irreversible step in the case of both organometallic compounds 1A and 1B. Both compounds also showed a remarkable selectivity towards AKR1C1 and AKR1C3 which are targets for breast cancer drug design. The organoruthenium complex of ligand pyrithione as well as pyrithione itself also displayed toxicity on the hormone-dependent MCF-7 breast cancer cell line with EC50 values in the low micromolar range.
机译：制备了四种临床使用的锌离子载体巯氧吡啶锌及其氧类似物2-羟基吡啶N-氧化物的钌配合物，并作为醛基酮还原酶亚家族1C（AKR1C）的酶抑制剂进行了评估。在对接模拟的辅助下进行的动力学研究表明，对于有机金属化合物1A和1B而言，抑制的混合类型包括快速可逆步骤和缓慢不可逆步骤。两种化合物还显示出对作为乳腺癌药物设计目标的AKR1C1和AKR1C3的显着选择性。配体巯氧吡啶的有机钌配合物以及巯氧吡啶本身也对激素依赖性MCF-7乳腺癌细胞系表现出毒性，其EC50值在低微摩尔范围内。

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