Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line

Myung Ho Jung, Hwan Kim, Won Kyoung Choi, Mohammed I. El-Gamal, Jin Hun Park, Kyung Ho Yoo, Tae Bo Sim, So Ha Lee, Daejin Baek, Jung Mi Hah, Jung Hyuck Cho, Chang Hyun Oh

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46 Citations (Scopus)

Abstract

Synthesis of a new series of diarylureas and amides having pyrrolo[2,3-d]pyrimidine scaffold is described. Their in vitro antiproliferative activities against A375 human melanoma cell line and HS 27 fibroblast cell line were tested and the effect of substituents on pyrrolo[2,3-d]pyrimidine was investigated. The newly synthesized compounds, except N-acetyl derivatives (Id, Ie, and Im), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Iq and Ir having imidazole and morpholine moieties, respectively, showed the most potent antiproliferative activity against A375.

Original languageEnglish
Pages (from-to)6538-6543
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
Publication statusPublished - 2009 Dec 1

Keywords

  • A375
  • Antiproliferative activity
  • HS 27
  • Melanoma
  • Pyrrolo[2,3-d]pyrimidine

ASJC Scopus subject areas

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

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  • Cite this

    Jung, M. H., Kim, H., Choi, W. K., El-Gamal, M. I., Park, J. H., Yoo, K. H., Sim, T. B., Lee, S. H., Baek, D., Hah, J. M., Cho, J. H., & Oh, C. H. (2009). Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line. Bioorganic and Medicinal Chemistry Letters, 19(23), 6538-6543. https://doi.org/10.1016/j.bmcl.2009.10.051