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, Hang Mei Polly Leung, Alfred King Yin Lam, Albert Sun Chi Chan, Kim Hung Lam, Cheuk On Tang

Research output: Journal article publicationJournal articleAcademic researchpeer-review

97 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 MTS50range of 12.5-25 μg/mL) and Hep3B (with a MTS50range 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


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

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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