一种芳香烷胺类化合物的合成及体外抗肿瘤活性研究
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Synthesis and in vitro Antitumor Activity of Aromatic Alkylamine compounds
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    摘要:

    以二苯乙酸和4,4,-二(4-氟苯)氯丁烷作为原料,经过一系列偶联反应得到系列芳香烷胺类化合物,结构经1H-NMR,13C-NMR,MS确证。采用MTT法选用人类前列腺癌(DU145、PC3),乳腺癌细胞(MCF-7、MDB-MB-231、MDB-MB-453)和正常上皮细胞(926)进行体外活性测试。体外生物活性评价显示,T3、 T4具有良好的生物活性,其中T3对MDB-MB-231 T4 对MDB-MB-453的活性最佳(IC50分别为17.30, 19.07,μM)。但对正常上皮细胞杀伤效力大(IC50分别为19.20, 26.37, μM)。T7有一定的抗乳腺癌作用(IC50分别为52.03,49.74,30.09,μM),且对正常上皮细胞IC50>50μM。

    Abstract:

    A series of novel aromatic alkylamine compounds were designed and prepared from the starting materials of 1,1'-(4-chlorobutylidene)bis(4-flourobenzene) and dibenzoic acid through a serious of coupling reaction, and the structures were characterized by 1H NMR,13C NMR and MS. Biological evalua- tion in vitro were evaluated by human prostate cancer cells (DU145、PC3) , breast cancer cells (MCF-7、MDB-MB-231、MDB-MB-453) and 926 by MTT assay.The results indicates that T3 has the best biological activity for MDB-MB-231(IC50=17.30μM) as well as T4 (IC50=19.07μM). However, the IC50 of 926 cells were shown the high toxicity on normal epithelial cells (IC50: 19.20, 26.37, μM). Compounds T7 had inhibitory effect against breast cancer cells(IC50: 52.03, 49.74,30.09, μM) and had a low toxicity on 926 (IC50>50).

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刘盼和,王敬,胡叶敏,李雁武.一种芳香烷胺类化合物的合成及体外抗肿瘤活性研究[J].精细化工,2017,34(12):

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  • 收稿日期:2017-01-22
  • 最后修改日期:2017-04-12
  • 录用日期:2017-05-23
  • 在线发布日期: 2017-11-10
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