Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents
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8-hydroxy-2-quinolinecarbaldehyde, Antitumor, Hepatocellular carcinoma, Quinoline derivatives
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.
ACS Medicinal Chemistry Letters
Chan, S.,Chui, C.,Chan, S.,Kok, S.,Chan, D.,Tsoi, M.,Leung, P.,Lam, A.,Chan, A.,Lam, K.,& Tang, J. (2013). Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents. ACS Medicinal Chemistry Letters, 4 (2), 170-174. http://dx.doi.org/10.1021/ml300238z