Document Type

Journal Article

Authors

Sau Hing Chan, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Chung Hin Chui, Clinical Division, School of Chinese Medicine, Hong Kong Baptist UniversityFollow
Shun Wan Chan, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Stanton Hon Lun Kok, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Dessy Chan, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Miriam Yuen Tung Tsoi, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Polly Hang Mei Leung, Department of Health Technology and Informatics, Hong Kong Polytechnic University
Alfred King Yin Lam, Department of Pathology, Griffith Medical School, Griffith University
Albert Sun Chi Chan, President Office, Hong Kong Baptist UniversityFollow
Kim Hung Lam, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University
Johnny Cheuk On Tang, Department of Applied Biology and Chemical Technology, Lo Ka Chung Centre for Natural Anti-Cancer Drug Development, Hong Kong Polytechnic University

Department/Unit

School of Chinese Medicine

Title

Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents

Language

English

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 (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. © 2012 American Chemical Society.

Keywords

8-hydroxy-2-quinolinecarbaldehyde, antitumor, hepatocellular carcinoma, quinoline derivatives

Publication Date

2013

Source Publication Title

ACS Medicinal Chemistry Letters

Volume

4

Issue

2

Start Page

170

End Page

174

Publisher

American Chemical Society

DOI

10.1021/ml300238z

Link to Publisher's Edition

http://dx.doi.org/10.1021/ml300238z

ISSN (print)

19485875

ISSN (electronic)

19485875

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