title: Synthesis and biological evaluation of novel aliphatic amido-quaternary ammonium salts for anticancer chemotherapy: part I.
abstract: 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.
authors.affiliation: Translational Research Center for Protein Function Control, Department of Biotechnology, Yonsei University, Seongsan-ro, Seodaemun-gu, Seoul 120-749, Republic of Korea.
authors.forename: Jee Sun
authors.initials: JS
authors.lastname: Yang
authors.forename: Doona
authors.initials: D
authors.lastname: Song
authors.forename: Boah
authors.initials: B
authors.lastname: Lee
authors.forename: Won Jin
authors.initials: WJ
authors.lastname: Ko
authors.forename: Song-Kyu
authors.initials: SK
authors.lastname: Park
authors.forename: Misun
authors.initials: M
authors.lastname: Won
authors.forename: Kiho
authors.initials: K
authors.lastname: Lee
authors.forename: Hwan Mook
authors.initials: HM
authors.lastname: Kim
authors.forename: Gyoonhee
authors.initials: G
authors.lastname: Han
mesh_terms: D000577:Amides / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic; D017930:Genes, Reporter; D006801:Humans; D008156:Luciferases / Q000235:genetics / Q000378:metabolism; D010879:Piperazines / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D012492:Salts / Q000737:chemistry; D015398:Signal Transduction; D013329:Structure-Activity Relationship; D020743:rhoB GTP-Binding Protein / Q000819:agonists* / Q000235:genetics / Q000378:metabolism
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D010879:Piperazines; D000644:Quaternary Ammonium Compounds; D012492:Salts; D008156:Luciferases; D020743:rhoB GTP-Binding Protein