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

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29 Scopus citations


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 languageEnglish
Pages (from-to)3900-3908
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Issue number9
StatePublished - Sep 2011

Bibliographical note

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


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


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