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Title 

New synthetic aliphatic sulfonamido-quaternary ammonium salts as anticancer chemotherapeutic agents

Authors 

D SongJ S YangC OhS CuiBo Kyung KimMi Sun WonJ I LeeH M KimG Han

Publisher 

Elsevier

Issue Date 

2013

Citation 

European Journal of Medicinal Chemistry, vol. 69, no. 0, pp. 670-677

Keywords 

Aliphatic sulfonamido-quaternary ammonium saltsAnticancer chemotherapeutic agentsNSC126188Open-ring moiety of quaternary ammonium saltsPerifosineRhoB

Abstract 

RhoB is expressed during tumor cell proliferation, survival, invasion, and metastasis. In malignant progression, the expression levels of RhoB are commonly attenuated. RhoB is known to be linked to the regulation of the PI3K/Akt survival pathways. Based on aliphatic amido-quaternary ammonium salts that induce apoptosis via up-regulation of RhoB, we synthesized novel aliphatic sulfonamido-quaternary ammonium salts. These new synthetic compounds were evaluated for their biological activities using an in vitro RhoB promoter assay in HeLa cells, and in a growth inhibition assay using human cancer cell lines including PC-3, NUGC-3, MDA-MB-231, ACHN, HCT-15, and NCI-H23. Compound 5b (ethyl-dimethyl-{3-[methyl-(tetradecane-1-sulfonyl)-amino]-propyl}-ammonium; iodide) was the most promising anticancer agent in the series, based upon the potency of growth inhibition and RhoB promotion. These new aliphatic sulfonamido-quaternary ammonium salts could be a valuable series for development of new anticancer chemotherapeutic agents.

ISSN 

0223-5234

Link 

http://dx.doi.org/10.1016/j.ejmech.2013.09.022

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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