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药学学报  2013 

新型双氢青蒿素哌嗪-磺酰胺类化合物的合成、结构及生物活性

, PP. 1430-1435

Keywords: 双氢青蒿素,哌嗪衍生物,合成,单晶结构,生物活性

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Abstract:

以双氢青蒿素为起始原料,经酯化、胺化、酰化快速、高效地合成了7种新型磺酰胺类双氢青蒿素哌嗪衍生物。通过ir、1hnmr、13cnmr和hr-ms对所有化合物进行了结构确定。并用x-单晶衍射法对化合物3c进行了最终构型确证。同时,以cck-8法对部分化合物进行了体外hela细胞毒性测试,初步测试结果表明:目标化合物对hela细胞有明显的抑制细胞增殖、诱导其凋亡的细胞毒活性,ic50最优值为0.14μmol·l-1。

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