一种芳香烷胺类化合物的合成及体外抗肿瘤活性研究

Synthesis and in vitro Antitumor Activity of Aromatic Alkylamine compounds

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).