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http://dx.doi.org/10.5012/bkcs.2011.32.4.1209

Synthesis and Antiproliferative Activity of Pyridinylcarbonylpyrimidines Against Melanoma Cell Line  

Ahn, Hye-Mi (Life/Health Division, Korea Institute of Science and Technology)
Lee, Jun-A (Life/Health Division, Korea Institute of Science and Technology)
Kim, Hwan (Life/Health Division, Korea Institute of Science and Technology)
Oh, Chang-Hyun (Life/Health Division, Korea Institute of Science and Technology)
Lee, So-Ha (Life/Health Division, Korea Institute of Science and Technology)
Sim, Tae-Bo (Life/Health Division, Korea Institute of Science and Technology)
Hah, Jung-Mi (Department of Pharmacy, College of Pharmacy, Hanyang University)
Kim, Dong-Jin (Life/Health Division, Korea Institute of Science and Technology)
Yoo, Kyung-Ho (Life/Health Division, Korea Institute of Science and Technology)
Publication Information
Abstract
The synthesis of the series of pyrimidinylamines 1a-d and pyrimidinylureas 1e-u bearing a novel pyridinylcarbonylpyrimidine scaffold and their antiproliferative activities against A375 human melanoma cell line were described. Among them, three compounds 1e, 1h, and 1o showed superior antiproliferative activities to Sorafenib ($IC_{50}=5.5{\mu}M$) as a reference compound. In our series, urea compound 1o having 4-chloro-3-trifluoromethyl moiety on the benzene nucleus exhibited very good antiproliferative activity with $IC_{50}$ value of $1.4{\mu}M$.
Keywords
Pyridinylcarbonylpyrimidines; Antiproliferative activity; Melanoma cell line;
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