title: Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents.
abstract: This letter describes the preparation of quinoline derivatives and their cytotoxic potentials toward human carcinoma cell lines. Among the selected compounds, 8-hydroxy-2-quinolinecarbaldehyde (3) showed the best in vitro cytotoxicity against the human cancer cell lines, including MDA231, T-47D, Hs578t, SaoS2, K562, SKHep1 (with a MTS50 range of 12.5-25 μg/mL) and Hep3B (with a MTS50 range of 6.25±0.034 μg/mL). The in vivo antitumor activity of compound 3 on subcutenaous Hep3B hepatocellular carcinoma xenograft in athymic nude mice was then studied. The results showed that the dose of 10 mg/kg/day of compound 3 with intraperitoneal injection for 9 days totally abolished the growth of the xenograft tumor of Hep3B with no histological damage on vital organs as compared with the control. The experimental results suggested that compound 3 has a good potential as an antitumor agent.
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Sau Hing
authors.initials: SH
authors.lastname: Chan
authors.affiliation: Clinical Division, School of Chinese Medicine, Hong Kong Baptist University , Hong Kong SAR, People's Republic of China.
authors.forename: Chung Hin
authors.initials: CH
authors.lastname: Chui
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Shun Wan
authors.initials: SW
authors.lastname: Chan
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Stanton Hon Lun
authors.initials: SH
authors.lastname: Kok
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Dessy
authors.initials: D
authors.lastname: Chan
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Miriam Yuen Tung
authors.initials: MY
authors.lastname: Tsoi
authors.affiliation: Department of Health Technology & Informatics, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Polly Hang Mei
authors.initials: PH
authors.lastname: Leung
authors.affiliation: Department of Pathology, Griffith Medical School and Griffith Health Institute, Griffith University , Gold Coast, Queensland, Australia.
authors.forename: Alfred King Yin
authors.initials: AK
authors.lastname: Lam
authors.affiliation: The President Office, Hong Kong Baptist University , Hong Kong SAR, People's Republic of China.
authors.forename: Albert Sun Chi
authors.initials: AS
authors.lastname: Chan
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Kim Hung
authors.initials: KH
authors.lastname: Lam
authors.affiliation: State Key Laboratory of Chirosciences, State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Shenzhen), Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hong Kong SAR, People's Republic of China.
authors.forename: Johnny Cheuk On
authors.initials: JC
authors.lastname: Tang
keywords: 8-hydroxy-2-quinolinecarbaldehyde; antitumor; hepatocellular carcinoma; quinoline derivatives