New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line

Hee Jin Kim, Hye Jung Cho, Hwan Kim, Mohammed I. El-Gamal, Chang Hyun Oh, So Ha Lee, Taebo Sim, Jung Mi Hah, Kyung Ho Yoo

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

A series of new diarylurea and diarylamide derivatives possessing acet(benz)amidophenyl scaffold was synthesized. Their in vitro antiproliferative activity was tested against A375P human melanoma cell line. Compounds 1c,d and 2c,d showed the highest potencies with IC 50 values in sub-micromolar scale. In addition, compounds 1b,e,l and 2e,l were more potent than Sorafenib but with IC 50 values in micromolar range. Moreover, compound 2c was equipotent to Vemurafenib, and 2d showed higher potency than Vemurafenib against A375P. Molar refractometry calculation and ADME profiling of the highest potent four derivatives 1c,d and 2c,d are also reported.

Original languageEnglish
Pages (from-to)3269-3273
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number9
DOIs
Publication statusPublished - 2012 May 1

Keywords

  • A375P
  • Acet(benz)amidophenyl
  • Antiproliferative activity
  • Diarylamide
  • Diarylurea
  • Melanoma

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line'. Together they form a unique fingerprint.

  • Cite this