Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line

Jun A. Lee, Eun Joo Roh, Chang Hyun Oh, So Ha Lee, Taebo Sim, Jong Seung Kim, Kyung Ho Yoo

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Synthesis of a new series of quinolinylaminopyrimidines 1a-k and quinazolinylmethylaminopyrimidines 2a-i containing aminoquinoline and aminoquinazoline as hinge regions is described. Their in vitro antiproliferative activities against A375P human melanoma cell line were tested. Among them, compounds 1h and 1k exhibited the highest antiproliferative activities against A375P cell line with IC<inf>50</inf> values in sub-micromolar scale. Compounds 1i, 2b and 2g showed similar potency against A375P to Sorafenib as a reference compound. The representative compound 1h showed high, dose-dependent inhibition of MEK and ERK kinases.

Original languageEnglish
Pages (from-to)607-614
Number of pages8
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume30
Issue number4
DOIs
Publication statusPublished - 2015 Aug 1

Fingerprint

Melanoma
Aminoquinolines
MAP Kinase Kinase Kinases
Cell Line
Inhibitory Concentration 50
sorafenib
In Vitro Techniques

Keywords

  • Antiproliferative
  • MEK/ERK kinase inhibition
  • melanoma cell line
  • quinazoline
  • quinoline

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line. / Lee, Jun A.; Roh, Eun Joo; Oh, Chang Hyun; Lee, So Ha; Sim, Taebo; Kim, Jong Seung; Yoo, Kyung Ho.

In: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 30, No. 4, 01.08.2015, p. 607-614.

Research output: Contribution to journalArticle

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