Synthesis of 8‑Hydroxyquinoline Derivatives as Novel Antitumor Agents

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 MTS₅₀ range of 12.5–25 μg/mL) and Hep3B (with a MTS₅₀ 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