New diarylamides and diarylureas possessing 8-amino(acetamido)quinoline scaffold: Synthesis, antiproliferative activities against melanoma cell lines, kinase inhibition, and in silico studies

Eun Jeong Koh, Mohammed I. El-Gamal, Chang Hyun Oh, So Ha Lee, Taebo Sim, Garam Kim, Hong Seok Choi, Jun Hee Hong, Sang Gi Lee, Kyung Ho Yoo

Research output: Contribution to journalArticle

24 Citations (Scopus)


Synthesis of a new series of diarylureas and diarylamides possessing 4-aryl-8-amino(acetamido)quinoline scaffold is described. Their in vitro antiproliferative activities against ten melanoma cell lines were tested. Compounds 1l, 2l, 3c, and 4c showed the highest potency against A375P cell line with IC50 values in sub-micromolar scale. Compound 4c was equipotent to Vemurafenib against A375P. In addition, compounds 1l, 2a, and 2l showed high potency over the NCI-9 tested melanoma cell line panel. The IC50 values of compounds 1l and 2l were in 2-digit nanomolar scale over four and five cell lines, respectively. Compound 2l showed high, dose-dependent inhibition of ERK kinase. ADME profiling showed that compounds 1l, 2l, 3c, 4c, and 5b are estimated to be orally bioavailable.

Original languageEnglish
Pages (from-to)10-21
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - 2013 Jan 1



  • Antiproliferative activity
  • Diarylamide
  • Diarylurea
  • ERK kinase
  • Melanoma
  • Quinoline

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this