齐墩果酸和熊果酸衍生物的合成、表征及抗癌活性的研究

发布时间：2018-04-03 04:08

  本文选题：齐墩果酸　切入点：熊果酸　出处：《有机化学》2016年04期

【摘要】：根据拼合原理,以天然产物齐墩果酸和熊果酸作为先导化合物,通过丁二酸连接片段,在C-28位分别导入哌嗪、N-甲基哌嗪及吗啉片段,共设计、合成了12种未见文献报道的齐墩果酸和熊果酸衍生物.利用IR、1H NMR、13C NMR和HRMS等波谱技术对所合成的目标化合物进行了结构表征,并采用3-(4,5-二甲基-2-噻唑)-2,5-二苯基溴化四氮唑噻唑蓝(MTT)法观察其对癌细胞的抑制作用,结果表明化合物OA-4、OA-7、OA-8a、OA-8b、UA-4、UA-7、UA-8a和UA-8b对人乳腺癌细胞(MCF-7)、人宫颈癌细胞(Hela)和人肺腺癌细胞(A549)的抑制作用远优于先导化合物齐墩果酸和熊果酸,且OA-4,OA-7,UA-4和UA-7与阳性对照物Gefitinib的IC50值相当.
[Abstract]:According to the splicing principle, the natural products oleanolic acid and ursolic acid were used as the leading compounds, and the fragments of piperazine N-methylpiperazine and morpholine were introduced at C-28, respectively.Twelve derivatives of oleanolic acid and ursolic acid which have not been reported in literature have been synthesized.The structures of the target compounds were characterized by IR 1H NMR13 C NMR and HRMS spectra. The inhibitory effects of these compounds on cancer cells were observed by using the method of 3 ~ (4) O ~ (4) -dimethyl -2-thiazolium -2-diphenyl tetrazolium tetrazolyl thiazolyl blue (MTT).缁撴灉琛ㄦ槑鍖栧悎鐗㎡A-4,OA-7,OA-8a,OA-8b,UA-4,UA-7,UA-8a鍜孶A-8b瀵逛汉涔宠吅鐧岀粏鑳，

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