新型苊[1,2-e]-1,2,4-三嗪衍生物的合成及抗癌评价

Somayeh, Adibi, Sedeh, Mohammad, Kazem, Mohammadi, Masood, Fereidoonnezhad, A. Javid
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引用次数: 0

摘要

本文介绍了几种苯基肼衍生物8 (a-h)的简便合成方法。为此,硫代氨基脲与苊-9,10-醌缩合生成苊[1,2-e]-1,2,4-三嗪-9(8H)-硫酮。然后与氯化苄衍生物进行联氨反应,再与不同的苯甲醛衍生物进行反应,得到收率较高的9-(苯基亚氨基肼)-苊[1,2-e]-1,2,4-三嗪衍生物(8a-h)。研究了合成的化合物对乳腺癌(MCF-7)、卵巢癌(SKOV3)和肺癌(A549)等人癌细胞的细胞毒性。其中8b、8c和8h表现出中等至良好的活性。
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Synthesis and anticancer evaluation of novel acenaphtho [1,2-e]-1,2,4- triazine derivatives
In this paper, we present the convenient syntheses of some new phenyl hydrazin derivatives 8 (a-h). For this purpose, condensation of thiosemicarbazide and acenaphtylene -9,10-quinone was performed to form acenaphtho[1,2-e]-1,2,4-triazine-9(8H)-thiones . Afterwards, the subsequent reaction with benzyl chloride derivatives was subjected to hydrazine and, then, the reaction was proceeded with different benzaldehyde derivatives to achieve 9-(phenyl imino hydrazin)-acenaphtho[1,2-e]-1,2,4-triazine derivatives (8a-h) in good yield. The cytotoxicity of the synthesized compounds was also studied against human cancer cell lines including breast (MCF-7), ovarian (SKOV3) and lung (A549) cell lines. Among them 8b, 8c and 8h showed moderate to good activity.
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Eurasian Chemical Communications
Eurasian Chemical Communications CHEMISTRY, MULTIDISCIPLINARY-
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