The effect of heterocyclic substituent at C-3 position of 1-(4-methyl-piperazin-1-yl)isoquinolines on their anticancer activity

Q4 Biochemistry, Genetics and Molecular Biology

Biopolymers and Cell Pub Date : 2022-07-25 DOI:10.7124/bc.000a71

A. Konovalenko, V. Zhirnov, O. Shablykin, O. Shablykina, V. Moskvina, V. Brovarets

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引用次数: 0

Abstract

Aim. A comparative analysis of the anti-cancer activity of 1-(4-methylpiperazin-1-yl)isoqui-nolines with different heteroaromatic substituents in С-3 position: 2-methylthiazol-4-yl, 2-phenylthiazol-4-yl, 2-(pyridin-4-yl)thiazol-4-yl, imidazo[2,1- b ]thiazol-6-yl, quinoxalin-2-yl, 6,7-dimethylquinoxalin-2-yl. Methods. Biological tests; statistic methods. Results. In vitro screening of the anticancer activity showed that the derivatives with 2-phenylthiazol-4-yl, quinoxaline-2-yl, 6,7-dimethylquinoxalin-2-yl substituents demonstrated the highest level of anticancer activity; however, they were inferior to 2-(pyridin-4-yl)thiazol-4-yl. The product with the 2-methylthiazol-4-yl residue almost did not demonstrated cytotoxicity. Comparative analysis showed no significant correlation with known drugs; hence these compounds have specific molecular targets. Conclusions. The resulting 1-amino-3-hetarylisoquinolines are a promising class of compounds for anticancer drug development. The level and direction of the activity significantly depend on the nature of heterocyclic substituents.

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1-(4-甲基哌嗪-1-酰基)异喹啉类化合物C-3位杂环取代基对其抗癌活性的影响

目标在С-3位具有不同杂芳取代基的1-（4-甲基哌嗪-1-基）异喹啉类化合物的抗癌活性的比较分析：2-甲基噻唑-4-基、2-苯基噻唑-4-基和2-（吡啶-4-基）噻唑-4-基，咪唑并[2,1-b]噻唑-6-基、喹喔啉-2-基和6,7-二甲基喹喔啉2-基。方法。生物试验；统计方法。后果抗癌活性的体外筛选表明，具有2-苯基噻唑-4-基、喹喔啉-2-基、6,7-二甲基喹喔啉2-基取代基的衍生物表现出最高水平的抗癌活性；但是它们不如2-（吡啶-4-基）噻唑-4-基。具有2-甲基噻唑-4-基残基的产物几乎没有表现出细胞毒性。比较分析显示，与已知药物没有显著相关性；因此这些化合物具有特定的分子靶标。结论。所得到的1-氨基-3-杂芳基异喹啉是一类有前途的抗癌药物开发化合物。活性的水平和方向在很大程度上取决于杂环取代基的性质。

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来源期刊

Biopolymers and Cell Biochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (all)

CiteScore

1.10

自引率

0.00%

发文量

期刊介绍： “Biopolymer and cell” is published since 1985 at the Institute of Molecular Biology and Genetics NAS of Ukraine under the supervision of the National Academy of Sciences of Ukraine. Our journal covers a wide scope of problems related to molecular biology and genetics including structural and functional genomics, transcriptomics, proteomics, bioinformatics, biomedicine, molecular enzymology, molecular virology and immunology, theoretical bases of biotechnology, physics and physical chemistry of proteins and nucleic acids and bioorganic chemistry.