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Synthesis and Antiproliferative Activity of 3-[(R-Hydrazono)Methyl]Cyclobutane-1,1,2,2-Tetracarbonitriles and 3-[(2-R-Hydrazono)Methyl]-6-Methylcyclohex-4-Ene-1,1,2,2-Tetracarbonitriles
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2020-06-01 , DOI: 10.1007/s11094-020-02183-1
M. A. Mar’yasov , V. V. Davydova , O. E. Nasakin , K. A. Lysenko

Aseries of cyclobutane-1,1,2,2-tetracarbonitriles contained a compound with significant activity against various cancer cell lines. The compound featured a thiosemicarbazide and the α,β-unsaturated aldehyde myrtenal in its structure and showed the highest activity against leukemia cells, the average growth inhibition against which was 88%. The proposed mechanism of action was associated with alkylation of the nucleophilic regions of tumor-cell DNA. The results showed that compounds with an ethyl-1,1,2,2-tetracarbonitrile fragment inhibited proliferation of malignant cells.

中文翻译:

3-[(R-Hydrazono)Methyl]Cyclobutane-1,1,2,2-Tetracarbonitriles 和 3-[(2-R-Hydrazono)Methyl]-6-Methylcyclohex-4-Ene-1 的合成和抗增殖活性, 1,2,2-四甲腈

一系列环丁烷-1,1,2,2-四甲腈含有一种对各种癌细胞系具有显着活性的化合物。该化合物以氨基硫脲和α,β-不饱和醛桃金娘醛为特征,对白血病细胞的活性最高,平均生长抑制率为88%。所提出的作用机制与肿瘤细胞 DNA 的亲核区域的烷基化有关。结果表明,含有乙基-1,1,2,2-四甲腈片段的化合物可抑制恶性细胞的增殖。
更新日期:2020-06-01
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