title: Synthesis of quinolinylaminopyrimidines and quinazolinylmethylaminopyrimidines with antiproliferative activity against melanoma cell line.
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 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.
authors.affiliation: Chemical Kinomics Research Center, Korea Institute of Science and Technology , Cheongryang, Seoul , Republic of Korea .
authors.forename: Jun A
authors.initials: JA
authors.lastname: Lee
authors.forename: Eun Joo
authors.initials: EJ
authors.lastname: Roh
authors.forename: Chang-Hyun
authors.initials: CH
authors.lastname: Oh
authors.forename: So Ha
authors.initials: SH
authors.lastname: Lee
authors.forename: Taebo
authors.initials: T
authors.lastname: Sim
authors.forename: Jong Seung
authors.initials: JS
authors.lastname: Kim
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Yoo
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D008545:Melanoma / Q000473:pathology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011743:Pyrimidines
keywords: Antiproliferative; MEK/ERK kinase inhibition; melanoma cell line; quinazoline; quinoline