Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives

Hee Kyung Rhee; Ji Hye Yoo; Eunyoung Lee; Young Joo Kwon; Hang Rhan Seo; Yun Sil Lee; Hea Young Park Choo

doi:10.1016/j.ejmech.2011.05.061

Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives

Hee Kyung Rhee, Ji Hye Yoo, Eunyoung Lee, Young Joo Kwon, Hang Rhan Seo, Yun Sil Lee, Hea Young Park Choo

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

29 Scopus citations

Abstract

Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.

Original language	English
Pages (from-to)	3900-3908
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	9
DOIs	https://doi.org/10.1016/j.ejmech.2011.05.061
State	Published - Sep 2011

Bibliographical note

Funding Information:
This work was supported by a grant (314-2008-1-E00306) from Korea Research Foundation.

Keywords

2-Phenylquinazolin-4(3H)-one
Cell cycle arrest
Cytotoxicity

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10.1016/j.ejmech.2011.05.061

Cite this

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title = "Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives",

abstract = "Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.",

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author = "Rhee, {Hee Kyung} and Yoo, {Ji Hye} and Eunyoung Lee and Kwon, {Young Joo} and Seo, {Hang Rhan} and Lee, {Yun Sil} and Choo, {Hea Young Park}",

note = "Funding Information: This work was supported by a grant (314-2008-1-E00306) from Korea Research Foundation.",

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doi = "10.1016/j.ejmech.2011.05.061",

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T1 - Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives

AU - Rhee, Hee Kyung

AU - Yoo, Ji Hye

AU - Lee, Eunyoung

AU - Kwon, Young Joo

AU - Seo, Hang Rhan

AU - Lee, Yun Sil

AU - Choo, Hea Young Park

N1 - Funding Information: This work was supported by a grant (314-2008-1-E00306) from Korea Research Foundation.

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N2 - Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.

AB - Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.

KW - 2-Phenylquinazolin-4(3H)-one

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KW - Cytotoxicity

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IS - 9

ER -

Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives

Abstract

Bibliographical note

Keywords

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