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新型α-氨基膦酸酯的合成与抗增殖活性

Synthesis and antiproliferative activity of novel α-aminophosphonates.

作者信息

Mungara Anil Kumar, Park Yong-Ki, Lee Kap Duk

机构信息

Department of Nanomaterial Chemistry, Dongguk University, Gyeongju 780–714, South Korea.

出版信息

Chem Pharm Bull (Tokyo). 2012;60(12):1531-7. Epub 2012 Sep 14.

Abstract

A novel series of carbazole-based α-aminophosphonates were synthesized by three component coupling of 6-bromo-9-ethyl-9H-carbazole-3-carbaldehyde, amine and diethyl phosphite using polyethylene glycol (PEG-400) as a green reaction media. The antiproliferative activity of these molecules was evaluated against three cancer cell lines. Of these, compounds 4c, 4e and 4m were found to exhibit good antiproliferative activity against three cancer cells, A549, MCF-7, and NCI-N87.

摘要

以聚乙二醇(PEG - 400)作为绿色反应介质,通过6 - 溴 - 9 - 乙基 - 9H - 咔唑 - 3 - 甲醛、胺和亚磷酸二乙酯的三组分偶联反应,合成了一系列新型咔唑基α - 氨基膦酸酯。评估了这些分子对三种癌细胞系的抗增殖活性。其中,发现化合物4c、4e和4m对三种癌细胞A549、MCF - 7和NCI - N87表现出良好的抗增殖活性。

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