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

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초록

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. (C) 2013 Elsevier Masson SAS. All rights reserved.

키워드

Aliphatic amido-quaternary ammonium salts; Open-ring form of aliphatic amido-quaternary ammonium salts; RhoB; GTPase RAt Sarcoma (Ras); Perifosine; NSC126188; RHOB EXPRESSION; RAS TRANSFORMATION; PROTEIN-KINASES; HUMAN CANCER; APOPTOSIS; CELLS; INHIBITORS
제목
Synthesis and biological evaluation of novel aliphatic amido-quaternary ammonium salts for anticancer chemotherapy: Part II
저자
Yang, Jee Sun; Song, Doona; Ko, Won Jin; Kim, Bunyea; Kim, Bo-Kyung; Park, Song-Kyu; Won, Misun; Lee, Kiho; Lee, Kyeong; Kim, Hwan Mook; Han, Gyoonhee
DOI
10.1016/j.ejmech.2012.12.063
발행일
2013-05
유형
Article
저널명
European Journal of Medicinal Chemistry
권
63
페이지
621 ~ 628