Synthesis and biological evaluation of novel aliphatic amido-quaternary ammonium salts for anticancer chemotherapy: Part I

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• 作者：Jee Sun Yang ; Doona Song ; Boah Lee ; Won Jin Ko ; Song-Kyu Park ; Misun Won ; Kiho Lee ; Hwan Mook Kim ; Gyoonhee Han
• 关键词：Aliphatic amido-quaternary ammonium salts ; RhoB ; GTPase RAt Sarcoma (Ras) ; Perifosine ; Piperazine alkyl derivatives ; NSC126188
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：July 2011
• 年：2011
• 卷：46
• 期：7
• 页码：2861-2866
• 全文大小：326 K

文摘

We synthesized novel aliphatic amido-quaternary ammonium salts in an effort to discover anticancer agents that increase Ras homolog gene family, member B, (RhoB) levels. These compounds exert anti-proliferative activities against several human cancer cell types. Seventeen compounds, varying in aliphatic carbon chain length and N-substituents, were synthesized and their biological activities were evaluated. Of these 17 compounds, compound 3i emerged as the most promising anticancer compound by promoting apoptosis through the RhoB mediated pathway. Potent biological activities observed for these novel aliphatic amido-quaternary ammonium salt analogues support their potential as anticancer, chemotherapeutic agents.