Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

Junsang Lee, Bong Soo Nam, Hwan Kim, Chang Hyun Oh, So Ha Lee, Seung Joo Cho, Taebo Sim, Jung Mi Hah, Dong Jin Kim, Jinsung Tae, Kyung Ho Yoo

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Abstract

The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC 50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.

Original languageEnglish
Pages (from-to)5722-5725
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
DOIs
Publication statusPublished - 2010 Oct 1

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Keywords

  • A375 human melanoma cell line
  • Aminoquinazolines
  • Antiproliferative activity
  • Selectivity
  • Synthesis

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Lee, J., Nam, B. S., Kim, H., Oh, C. H., Lee, S. H., Cho, S. J., Sim, T., Hah, J. M., Kim, D. J., Tae, J., & Yoo, K. H. (2010). Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line. Bioorganic and Medicinal Chemistry Letters, 20(19), 5722-5725. https://doi.org/10.1016/j.bmcl.2010.08.010