2. Academic Validation
  3. Design, synthesis and biological evaluation of novel aliphatic amido/sulfonamido-quaternary ammonium salts as antitumor agents

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

  • Bioorg Med Chem. 2013 Feb 1;21(3):788-94. doi: 10.1016/j.bmc.2012.11.027.
Doona Song 1,  Jee Sun Yang,  Seo Joong Kim,  Bo-Kyung Kim,  Song-Kyu Park,  Misun Won,  Kiho Lee,  Hwan Mook Kim,  Kang-Yell Choi,  Kyeong Lee,  Gyoonhee Han
Affiliations

Affiliation

  • 1 Translational Research Center for Protein Function Control, Department of Biotechnology, Yonsei University, Seoul 120-749, Republic of Korea.
PMID: 23266181 DOI: 10.1016/j.bmc.2012.11.027
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.

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