嘧啶嘧啶嘧啶和三唑嘧啶嘧啶嘧啶衍生物:人类癌细胞系的合成和细胞毒性评价。

Seyed-Hadi Mousavi, Hoda Atapour-Mashhad, Mehdi Bakavoli, Ali Shiri, Marzieh Akbarzadeh, Zahra Tayarani-Najaran
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引用次数: 0

摘要

研究了几种嘧啶[4,5-e][1,3,4]恶二嗪和[1,2,4]三唑[4',3':1,2]嘧啶[4,5-e][1,3,4]恶二嗪衍生物对人恶性癌细胞的体外抗增殖活性。所有合成的化合物均以剂量依赖性方式抑制恶性细胞的生长,但其中具有三唑基团的1,5,7-三甲基-3-苯基- 1h -[1,2,4]三唑[4',3':1,2]嘧啶[4,5-e][1,3,4]三唑[4',3':1,2]嘧啶[4,5-e][1,3,4]恶二嗪-[1,2,4]三唑[4',3':1,2]嘧啶[4,5-e][1,3,4]恶二嗪-7-基)磺酰基]乙腈的抑制效果较好;与对照组相比,它们还在处理细胞的流式细胞术直方图中诱导了一个亚g1峰,表明它们诱导的毒性涉及凋亡细胞死亡。结果表明,含三唑基团与嘧啶[4,5-e][1,3,4]恶二嗪衍生物熔接的化合物比含C-7位氯或吡咯烷基团的化合物活性更高。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PYRIMIDOOXADIAZINE AND TRIAZOLOPYRIMIDOOXADIAZINE DERIVATIVES: SYNTHESIS AND CYTOTOXIC EVALUATION IN HUMAN CANCER CELL LINES.

In vitro antiproliferative activities of some pyrimido[4,5-e][1,3,4]oxadiazine and [1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazine derivatives were examined in human malignant cancer cell lines. All synthesized compounds inhibited the growth of malignant cells in a dose dependent manner, but among them 1,5,7-trimethyl-3-phenyl-1H-[1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazine and [(1,5-dimethyl-3-phenyl-1H-[1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazin-7-yl)sulfanyl]acetonitrile, both with triazole moiety, were found to be more effective than other compounds; they also induced a sub-G1 peak in the flow cytometry histogram of treated cells compared to controls, indicating that apoptotic cell death is involved in toxicity they induce. The results showed that compounds with triazole moiety fused to pyrimido[4,5-e] [1,3,4]oxadiazine derivatives are more active than those bearing chlorine or pyrrolidine groups at C-7 position.

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