TY - JOUR
T1 - Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents
AU - Chan, Sau Hing
AU - CHUI, Chung Hin
AU - Chan, Shun Wan
AU - Kok, Stanton Hon Lun
AU - Chan, Dessy
AU - Tsoi, Miriam Yuen Tung
AU - Leung, Polly Hang Mei
AU - Lam, Alfred King Yin
AU - Chan, Albert Sun Chi
AU - Lam, Kim Hung
AU - Tang, Johnny Cheuk On
N1 - This work is also supported by (i) the General Research Fund (grant no. PolyU 5001/09P) offered by the RGC of HKSAR, (ii) the AoE Scheme established under the UGC of HKSAR (Project No. AoE/P-10/01), and (iii) the Shenzhen Municipal Key Laboratory Advancement Program 2008, Shenzhen
PY - 2013/2/14
Y1 - 2013/2/14
N2 - 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.
AB - 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.
KW - 8-hydroxy-2-quinolinecarbaldehyde
KW - antitumor
KW - hepatocellular carcinoma
KW - quinoline derivatives
UR - https://www.scopus.com/pages/publications/84873963908
U2 - 10.1021/ml300238z
DO - 10.1021/ml300238z
M3 - Journal article
AN - SCOPUS:84873963908
SN - 1948-5875
VL - 4
SP - 170
EP - 174
JO - ACS Medicinal Chemistry Letters
JF - ACS Medicinal Chemistry Letters
IS - 2
ER -
