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

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Title
New synthetic aliphatic sulfonamido-quaternary ammonium salts as anticancer chemotherapeutic agents
Author(s)
D Song; J S Yang; C Oh; S Cui; Bo Kyung KimMi Sun Won; J I Lee; H M Kim; G Han
Bibliographic Citation
European Journal of Medicinal Chemistry, vol. 69, pp. 670-677
Publication Year
2013
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.
Keyword
Aliphatic sulfonamido-quaternary ammonium saltsAnticancer chemotherapeutic agentsNSC126188Open-ring moiety of quaternary ammonium saltsPerifosineRhoB
ISSN
0223-5234
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.ejmech.2013.09.022
Type
Article
Appears in Collections:
Division of Biomedical Research > Personalized Genomic Medicine Research Center > 1. Journal Articles
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