Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents

Sau Hing Chan, Chung Hin CHUI, Shun Wan Chan, Stanton Hon Lun Kok, Dessy Chan, Miriam Yuen Tung Tsoi, Polly Hang Mei Leung, Alfred King Yin Lam, Albert Sun Chi Chan*, Kim Hung Lam, Johnny Cheuk On Tang

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

100 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)170-174
Number of pages5
JournalACS Medicinal Chemistry Letters
Issue number2
Publication statusPublished - 14 Feb 2013

Scopus Subject Areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • 8-hydroxy-2-quinolinecarbaldehyde
  • antitumor
  • hepatocellular carcinoma
  • quinoline derivatives


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