title: Design and synthesis of 2-(3-alkylaminophenyl)-6-(pyrrolidin-1-yl)quinolin-4-ones as potent antitumor agents.
abstract: 2-(3-Alkylaminophenyl)-6-(pyrrolidin-1-yl)quinolin-4-ones 1-3 were synthesized and screened for anti-proliferative activity against three human cancer cell lines, as well as the normal cell line Detroit 551. All of the synthesized target compounds 1-3 demonstrated potent cytotoxic activity against the cancer cell lines, but weak inhibitory activity toward the normal cell line. 2-(3-Methyl aminophenyl)-6-(pyrrolidin-1-yl)quinolin-4-one (1), one of the potent compounds in vitro, was also tested in an in vivo Hep3B xenograft nude mice model, and its significant anticancer activity was reconfirmed. Therefore, compound 1 merits further investigation as an antitumor clinical trial candidate and potential anticancer agent.
authors.affiliation: Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung 404, Taiwan.
authors.forename: Shih-Ming
authors.initials: SM
authors.lastname: Huang
authors.forename: Yung-Yi
authors.initials: YY
authors.lastname: Cheng
authors.forename: Ming-Hua
authors.initials: MH
authors.lastname: Chen
authors.forename: Chi-Hung
authors.initials: CH
authors.lastname: Huang
authors.forename: Li-Jiau
authors.initials: LJ
authors.lastname: Huang
authors.forename: Mei-Hua
authors.initials: MH
authors.lastname: Hsu
authors.forename: Sheng-Chu
authors.initials: SC
authors.lastname: Kuo
authors.forename: Kuo-Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D011759:Pyrrolidines; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D023041:Xenograft Model Antitumor Assays
chemical_list: C559958:2-(3-(methylamino)phenyl)-6-(pyrrolidin-1-yl)quinolin-4-one; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D011759:Pyrrolidines; D015363:Quinolones