Synthesis of 8-Hydroxyquinoline Derivatives as Novel Antitumor Agents
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- 作者：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
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：February 14, 2013
- 年：2013
- 卷：4
- 期：2
- 页码：170-174
- 全文大小：359K
- 年卷期：v.4,no.2(February 14, 2013)
- ISSN：1948-5875
文摘
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鈥?5 渭g/mL) and Hep3B (with a MTS50 range of 6.25卤0.034 渭g/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.