Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents

Sau Hing Chan; Chung Hin Chui; Shun Wan Chan; Stanton Hon Lun Kok; Dessy Chan; Miriam Yuen Tung Tsoi; Hang Mei Polly Leung; Alfred King Yin Lam; Albert Sun Chi Chan; Kim Hung Lam; Cheuk On Tang

doi:10.1021/ml300238z

Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents

Sau Hing Chan, Chung Hin Chui, Shun Wan Chan, Stanton Hon Lun Kok, Dessy Chan, Miriam Yuen Tung Tsoi, Hang Mei Polly Leung, Alfred King Yin Lam, Albert Sun Chi Chan, Kim Hung Lam, Cheuk On Tang

Research output: Journal article publication › Journal article › Academic research › peer-review

116 Citations (Scopus)

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 MTS50range of 12.5-25 μg/mL) and Hep3B (with a MTS50range 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.

Original language	English
Pages (from-to)	170-174
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	4
Issue number	2
DOIs	https://doi.org/10.1021/ml300238z
Publication status	Published - 14 Feb 2013

Keywords

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

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1021/ml300238z

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title = "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 (3) showed the best in vitro cytotoxicity against the human cancer cell lines, including MDA231, T-47D, Hs578t, SaoS2, K562, SKHep1 (with a MTS50range of 12.5-25 μg/mL) and Hep3B (with a MTS50range 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.",

keywords = "8-hydroxy-2-quinolinecarbaldehyde, antitumor, hepatocellular carcinoma, quinoline derivatives",

author = "Chan, \{Sau Hing\} and Chui, \{Chung Hin\} and Chan, \{Shun Wan\} and Kok, \{Stanton Hon Lun\} and Dessy Chan and Tsoi, \{Miriam Yuen Tung\} and Leung, \{Hang Mei Polly\} and Lam, \{Alfred King Yin\} and Chan, \{Albert Sun Chi\} and Lam, \{Kim Hung\} and Tang, \{Cheuk On\}",

year = "2013",

month = feb,

day = "14",

doi = "10.1021/ml300238z",

language = "English",

volume = "4",

pages = "170--174",

journal = "ACS Medicinal Chemistry Letters",

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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, Hang Mei Polly

AU - Lam, Alfred King Yin

AU - Chan, Albert Sun Chi

AU - Lam, Kim Hung

AU - Tang, Cheuk On

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 MTS50range of 12.5-25 μg/mL) and Hep3B (with a MTS50range 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 MTS50range of 12.5-25 μg/mL) and Hep3B (with a MTS50range 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

SN - 1948-5875

VL - 4

SP - 170

EP - 174

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 2

ER -

Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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