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.
|Number of pages||8|
|Journal||Journal of Enzyme Inhibition and Medicinal Chemistry|
|Publication status||Published - 2015 Aug 1|
- MEK/ERK kinase inhibition
- melanoma cell line
ASJC Scopus subject areas
- Drug Discovery