Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines. Part 2

Myung Ho Jung, Mohammed I. El-Gamal, Mohammed S. Abdel-Maksoud, Taebo Sim, Kyung Ho Yoo, Chang Hyun Oh

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

A new series of diarylureas and diarylamides possessing 1H-pyrrolo[3,2-c]pyridine scaffold was designed and synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-9 human melanoma cell line panel were tested. All the target compounds, except three amino derivatives 8g, h and 9h, demonstrated superior potencies against A375P to Sorafenib. In addition, compounds 8a and 9b-f demonstrated higher potencies than Vemurafenib against A375P. Compounds 8c and 9b were 7.50 and 454.90 times, respectively, more selective towards A375P melanoma cells over NIH3T3 fibroblasts. Furthermore, compounds 8d, e and 9a-d, f demonstrated very high potencies against the nine tested melanoma cell lines at the NCI. The bisamide derivatives 9a-c, f showed 2-digit nanomolar IC 50 values over different cell lines of the NCI-9 melanoma cell lines.

Original languageEnglish
Pages (from-to)4362-4367
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number13
DOIs
Publication statusPublished - 2012 Jul 1

Keywords

  • A375P
  • Antiproliferative activity
  • Diarylamide
  • Diarylurea
  • Melanoma
  • Pyrrolo[3,2-c]pyridine

ASJC Scopus subject areas

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

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