School of Chinese Medicine
Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents
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. © 2012 American Chemical Society.
8-hydroxy-2-quinolinecarbaldehyde, antitumor, hepatocellular carcinoma, quinoline derivatives
Source Publication Title
ACS Medicinal Chemistry Letters
American Chemical Society
Link to Publisher's Edition
Chan, Sau Hing, 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, and Johnny Cheuk On Tang. "Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents." ACS Medicinal Chemistry Letters 4.2 (2013): 170-174.