Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

Serebryanskaya Tatiyana V.; Lyakhov Alexander S.; Ivashkevich Ludmila S.; Schur Julia; Frias Corazon; Prokop Aram; Ott Ingo

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Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

机译：硫代四唑酸金（I）作为硫氧还蛋白还原酶抑制剂和抗增殖剂

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Gold(I) complexes with phosphane and thiotetrazolate ligands were prepared and investigated as a new type of bioactive gold metallodrugs. The complexes triggered very efficient inhibition of the enzyme thioredoxin reductase (TrxR), which is an important molecular target for gold species. Strong cytotoxic effects were observed in MDA-MB-231 breast adenocarcinoma and HT-29 colon carcinoma cells, and the complexes also caused strong effects in vincristine resistant Nalm-6 leukemia cells. Cellular uptake studies showed elevated cellular gold levels for complexes containing a triphenylphosphane ligand, whereas trifurylphosphane analogues accumulated at significantly lower cellular concentrations.

机译：制备了具有膦和硫代四唑配体的金（I）配合物，并将其作为新型的生物活性金金属药物进行了研究。该配合物触发了对硫氧还蛋白还原酶（TrxR）的非常有效的抑制，该酶是金物种的重要分子靶标。在MDA-MB-231乳腺癌和HT-29结肠癌细胞中观察到了强烈的细胞毒性作用，并且该复合物在耐长春新碱的Nalm-6白血病细胞中也产生了强大的作用。细胞摄取研究表明，含有三苯基膦配体的配合物的细胞金水平升高，而三呋喃膦类似物以明显较低的细胞浓度积累。

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《Dalton transactions: An international journal of inorganic chemistry》 |2015年第3期|共9页
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Serebryanskaya Tatiyana V.; Lyakhov Alexander S.; Ivashkevich Ludmila S.; Schur Julia; Frias Corazon; Prokop Aram; Ott Ingo;
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1. Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents [J] . Serebryanskaya Tatiyana V., Lyakhov Alexander S., Ivashkevich Ludmila S., Dalton transactions: An international journal of inorganic chemistry . 2015,第3期

机译：硫代四唑酸金（I）作为硫氧还蛋白还原酶抑制剂和抗增殖剂
2. Applying the designed multiple ligands approach to inhibit dihydrofolate reductase and thioredoxin reductase for antiproliferative activity [J] . Ng Hu-Li, Chen Shangying, Chew Eng-Hui, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2016,第Null期

机译：应用设计的多配体方法抑制二氢叶酸还原酶和硫氧还蛋白还原酶的抗增殖活性
3. Gold(I) NHC Complexes: Antiproliferative Activity, Cellular Uptake, Inhibition of Mammalian and Bacterial Thioredoxin Reductases, and Gram-Positive Directed Antibacterial Effects [J] . Claudia Schmidt, Bianka Karge, Rainer Misgeld, Chemistry: A European journal . 2017,第8期

机译：黄金（i）NHC复合物：抗增殖活性，细胞吸收，哺乳动物抑制和细菌硫氧嗪还原酶，以及革兰氏阳性定向抗菌作用
4. Identification of Plasmodium falciparum thioredoxin reductase (PfTrxR) inhibitors from Malaria Box using LC-MS functional assay [C] . Angela I. Calderon, Neil Tiwari, Katja Becker ASMS Conference on Mass Spectrometry and Allied Topics . 2014

机译：使用LC-MS功能测定法鉴定来自疟疾盒的疟原虫氧化嗪（PFTRXR）抑制剂
5. The role of the mitochondrial thioredoxin/thioredoxin reductase antioxidant system in dopaminergic cell death [D] . Lopert, Pamela Nancy 2014

机译：线粒体硫氧还蛋白/硫氧还蛋白还原酶抗氧化剂系统在多巴胺能细胞死亡中的作用
6. Metal- and Semimetal-Containing Inhibitors of Thioredoxin Reductase as Anticancer Agents [O] . Valentina Gandin, Aristi P. Fernandes 2015

机译：硫氧还蛋白还原酶的金属和半金属抑制剂作为抗癌药
7. Metal- and semimetal-containing inhibitors of thioredoxin reductase as anticancer agents [O] . Gandin, Valentina, Fernandes, Aristi P. 2015

机译：含金属和半金属的硫氧还蛋白还原酶抑制剂作为抗癌药

Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

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