Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma

Hee Jin Kim, Myung Ho Jung, Hwan Kim, Mohammed I. El-Gamal, Taebo Sim, So Ha Lee, Jun Hee Hong, Jung Mi Hah, Jung Hyuck Cho, Jung Hoon Choi, Kyung Ho Yoo, Chang Hyun Oh

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32 Citations (Scopus)

Abstract

Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375.

Original languageEnglish
Pages (from-to)413-417
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number1
DOIs
Publication statusPublished - 2010 Jan 1

Keywords

  • A375
  • Antiproliferative activity
  • HS 27
  • Melanoma
  • Pyrrolo[3,2-b]pyridine

ASJC Scopus subject areas

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

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  • Cite this

    Kim, H. J., Jung, M. H., Kim, H., El-Gamal, M. I., Sim, T., Lee, S. H., Hong, J. H., Hah, J. M., Cho, J. H., Choi, J. H., Yoo, K. H., & Oh, C. H. (2010). Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma. Bioorganic and Medicinal Chemistry Letters, 20(1), 413-417. https://doi.org/10.1016/j.bmcl.2009.08.005