Translational Research Center for Protein Function Control, Department of Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.
Eur J Med Chem. 2013 May;63:621-8. doi: 10.1016/j.ejmech.2012.12.063. Epub 2013 Mar 14.
A series of novel aliphatic amido-quaternary ammonium salts were synthesized and evaluated for their anticancer effects involving induction of RhoB. Most of these compounds, featuring open-ring forms of aliphatic amido-quaternary ammonium salts, exhibited potent anti-proliferative activities in human cancer cell lines, including PC-3, NUGC-3, MDA-MB-231, ACHN, HCT-15, and NCI-H23. In further evaluation, the representative compound N,N-diethyl-N-(2-(N-methyltetradecanamido)ethyl)prop-2-en-1-aminium bromide (3b) exhibited potent pro-apoptotic activity, through RhoB activation, in HeLa cells.
一系列新型脂肪族酰胺季铵盐被合成并评价了其诱导 RhoB 表达的抗癌效果。这些化合物大多具有脂肪族酰胺季铵盐的开环形式，在包括 PC-3、NUGC-3、MDA-MB-231、ACHN、HCT-15 和 NCI-H23 的人癌细胞系中表现出很强的抗增殖活性。在进一步的评价中，代表性化合物 N,N-二乙基-N-(2-(N-甲基十四烷酰胺基)乙基)丙-2-烯-1-胺溴盐（3b）通过 RhoB 的激活，在 HeLa 细胞中表现出很强的促凋亡活性。
