Synthesis of Quinolinylaminopyrimidines and Quinazolinylmethylaminopyrimidines with Antiproliferative Activity against Melanoma Cell Line
- Synthesis of Quinolinylaminopyrimidines and Quinazolinylmethylaminopyrimidines with Antiproliferative Activity against Melanoma Cell Line
- 이준아; 노은주; 오창현; 이소하; 심태보; 김종승; 유경호
- Melanoma cell line; Quinazoline; Quinoline; Antiproliferative; MEK/ERK kinase inhibition
- Issue Date
- Journal of enzyme inhibition and medicinal chemistry
- VOL 30, NO 4, 607-614
- 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 IC50 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.
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