脱氢二乙胺和金刚烷的新衍生物：作为修复酶 TDP1 抑制剂的合成和活性

IF 1.7 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Russian Chemical Bulletin Pub Date : 2024-07-26 DOI:10.1007/s11172-024-4300-0

K. S. Kovaleva, O. I. Yarovaya, I. A. Chernyshova, O. I. Lavrik, N. F. Salakhutdinov

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引用次数: 0

摘要

为了研究连接体类型和长度对生物活性的影响，我们采用三步合成法获得了脱氢二乙胺和金刚烷的一些新共轭物。研究了合成化合物对 DNA 修复酶酪氨酰-DNA 磷酸二酯酶 1 的抑制活性。这些化合物是强效抑制剂，在微摩尔浓度下就具有活性。

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New derivatives of dehydroabiethylamine and adamantane: synthesis and activity as inhibitors of the repair enzyme TDP1

A number of new conjugates of dehydroabiethylamine and adamantane was obtained using a three-step synthetic scheme in order to study the effect of linker type and length on biological activity. The inhibitory activity of the synthesized compounds toward the DNA repair enzyme Tyrosyl-DNA phosphodiesterase 1 was studied. The compounds are potent inhibitors, exhibiting activity in micromolar concentrations.

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来源期刊

Russian Chemical Bulletin 化学-化学综合

CiteScore

2.70

自引率

47.10%

发文量

257

审稿时长

3-8 weeks

期刊介绍： Publishing nearly 500 original articles a year, by leading Scientists from Russia and throughout the world, Russian Chemical Bulletin is a prominent international journal. The coverage of the journal spans practically all areas of fundamental chemical research and is presented in five sections: General and Inorganic Chemistry; Physical Chemistry; Organic Chemistry; Organometallic Chemistry; Chemistry of Natural Compounds and Bioorganic Chemistry.