Synthesis of 8‑Hydroxyquinoline Derivatives as Novel Antitumor Agents

• Published in: ACS medicinal chemistry letters Vol. 4; no. 2; pp. 170 - 174
• Main Authors: Chan, Sau Hing, Chui, Chung Hin, Chan, Shun Wan, Kok, Stanton Hon Lun, Chan, Dessy, Tsoi, Miriam Yuen Tung, Leung, Polly Hang Mei, Lam, Alfred King Yin, Chan, Albert Sun Chi, Lam, Kim Hung, Tang, Johnny Cheuk On
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 14-02-2013
• Subjects: Letter; 8-hydroxy-2-quinolinecarbaldehyde; quinoline derivatives; antitumor; hepatocellular carcinoma
• ISSN: 1948-5875; 1948-5875
• DOI: 10.1021/ml300238z

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.