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Title 

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

Authors 

D SongJ S YangS J KimB K KimS K ParkMi Sun WonK LeeH M KimK Y ChoiG Han

Publisher 

Elsevier

Issue Date 

2013

Citation 

Bioorganic & Medicinal Chemistry, vol. 21, no. 3, pp. 788-794

Keywords 

Aliphatic amido/sulfonamido-quaternary ammonium saltsGTPase rat sarcoma (Ras)NSC126188PerifosineRhoB

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.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2012.11.027

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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