Design, synthesis and biological evaluation of novel aliphatic amido/sulfonamido-quaternary ammonium salts as antitumor agents

Doona Song, Jee Sun Yang, Seo Joong Kim, Bo Kyung Kim, Song Kyu Park, Misun Won, Hwan Mook Kim, Kang Yell Choi, Kyeong Lee, Kiho Lee, Gyoonhee Han

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

RhoB, one of the upstream signaling proteins of the phosphatidylinositol-3- kinase (PI3K)/Akt pathway, is frequently mutated in human cancer. Based on a piperazine alkyl derivative that induced apoptosis via up-regulation of RhoB, we synthesized novel aliphatic amido/sulfonamido-quaternary ammonium salts and evaluated their biological activities using an in vitro growth inhibition assay and RhoB promoter assay in human cancer cells. Compound 3a was the most promising anticancer agent in the series, based upon its potent growth inhibition via RhoB-mediated signaling. These novel aliphatic amido/sulfonamido-quaternary ammonium salts may be useful as a platform for development of anticancer chemotherapeutic agents.

Original languageEnglish
Pages (from-to)788-794
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number3
DOIs
Publication statusPublished - 2013 Feb 1

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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