Synthesis and biological evaluation of novel aliphatic amido-quaternary ammonium salts for anticancer chemotherapy: part II

Eur J Med Chem. 2013 May:63:621-8. doi: 10.1016/j.ejmech.2012.12.063.

Jee Sun Yang ¹, Doona Song, Won Jin Ko, Bunyea Kim, Bo-Kyung Kim, Song-Kyu Park, Misun Won, Kiho Lee, Kyeong Lee, Hwan Mook Kim, Gyoonhee Han

Affiliations

Affiliation

1 Translational Research Center for Protein Function Control, Department of Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.

PMID: 23567950 DOI: 10.1016/j.ejmech.2012.12.063

Abstract

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.

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