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.
Bibliographical noteFunding Information:
This research was supported by National Research Foundation ( 2012-0000884 ); Korean Research WCU grant ( R31-2008-000-10086-0 ); and the Brain Korea 21 Project of the Republic of Korea .
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry