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新型含 1-氨基四氢萘的脲类和磺胺类化合物的合成及抗癌活性。

Synthesis and Anticancer Activity of Novel Ureas and Sulfamides Incorporating 1-Aminotetralins.

机构信息

Department of Basic Sciences, Erzurum Technical University, Faculty of Science, Erzurum, Turkey.

Department of Basic Sciences, Erzurum Technical University, Faculty of Science, Erzurum, Turkey.

出版信息

Arch Med Res. 2017 Aug;48(6):513-519. doi: 10.1016/j.arcmed.2017.12.002. Epub 2017 Dec 14.

DOI:10.1016/j.arcmed.2017.12.002
PMID:29248174
Abstract

BACKGROUND AND AIMS

In the present study, a series of ureas and sulfamides derived from 1-aminotetralins were synthesized. For this purpose, urea and sulfamide analogues were synthesized from the reactions of substituted 1-aminotetralins with N,N-dimethylcarbamoyl chloride and N,N-dimethylsulfamoyl chloride. The anticancer activity of newly synthesized compounds was tested against human U-87MG glioblastoma and PC-3 prostate cancer cell lines. Cytotoxicity was examined using MTT and LDH release assays.

RESULTS

The obtained data revealed that tested compounds showed a variable degree of cytotoxic activity against the tested cell lines. 3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-1,1-dimethylurea (9) and 3-(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-1,1-dimethylurea (10) proved to be the most active cytotoxic members in this study.

CONCLUSIONS

These two compounds could be considered as possible anticancer agents.

摘要

背景与目的

在本研究中,我们合成了一系列衍生自 1-氨基四氢萘的脲和磺酰胺类化合物。为此,我们通过取代的 1-氨基四氢萘与 N,N-二甲基氨基甲酰氯和 N,N-二甲基磺酰胺酰氯的反应合成了脲和磺酰胺类似物。我们测试了新合成化合物对人 U-87MG 神经胶质瘤和 PC-3 前列腺癌细胞系的抗癌活性。使用 MTT 和 LDH 释放测定法检测细胞毒性。

结果

获得的数据表明,测试的化合物对测试的细胞系表现出不同程度的细胞毒性活性。3-(5-甲氧基-1,2,3,4-四氢萘-1-基)-1,1-二甲基脲(9)和 3-(6-甲氧基-1,2,3,4-四氢萘-1-基)-1,1-二甲基脲(10)被证明是本研究中最具活性的细胞毒性成员。

结论

这两种化合物可以被认为是有希望的抗癌药物。

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