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

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Ammonium Compounds
Antineoplastic Agents
Assays
Salts
Phosphatidylinositol 3-Kinase
Growth
Bioactivity
Neoplasms
Up-Regulation
Cells
Apoptosis
Derivatives
Proteins
piperazine
In Vitro Techniques

All Science Journal Classification (ASJC) codes

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

Cite this

Song, Doona ; Yang, Jee Sun ; Kim, Seo Joong ; Kim, Bo Kyung ; Park, Song Kyu ; Won, Misun ; Kim, Hwan Mook ; Choi, Kang Yell ; Lee, Kyeong ; Lee, Kiho ; Han, Gyoonhee. / Design, synthesis and biological evaluation of novel aliphatic amido/sulfonamido-quaternary ammonium salts as antitumor agents. In: Bioorganic and Medicinal Chemistry. 2013 ; Vol. 21, No. 3. pp. 788-794.
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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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Design, synthesis and biological evaluation of novel aliphatic amido/sulfonamido-quaternary ammonium salts as antitumor agents. / Song, Doona; Yang, Jee Sun; Kim, Seo Joong; Kim, Bo Kyung; Park, Song Kyu; Won, Misun; Kim, Hwan Mook; Choi, Kang Yell; Lee, Kyeong; Lee, Kiho; Han, Gyoonhee.

In: Bioorganic and Medicinal Chemistry, Vol. 21, No. 3, 01.02.2013, p. 788-794.

Research output: Contribution to journalArticle

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AU - Song, Doona

AU - Yang, Jee Sun

AU - Kim, Seo Joong

AU - Kim, Bo Kyung

AU - Park, Song Kyu

AU - Won, Misun

AU - Kim, Hwan Mook

AU - Choi, Kang Yell

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AU - Lee, Kiho

AU - Han, Gyoonhee

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