Synthesis of 8‑Hydroxyquinoline
Derivatives
as Novel Antitumor Agents
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Abstract
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 (<b>3</b>) showed the best <i>in vitro</i> cytotoxicity
against the human cancer cell lines, including MDA231, T-47D, Hs578t,
SaoS2, K562, SKHep1 (with a MTS<sub>50</sub> range of 12.5–25
μg/mL) and Hep3B (with a MTS<sub>50</sub> range of 6.25±0.034
μg/mL). The <i>in vivo</i> antitumor activity of compound <b>3</b> 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 <b>3</b> 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 <b>3</b> has a good potential as an antitumor agent