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http://dx.doi.org/10.5012/bkcs.2010.31.10.2854

Synthesis of New 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b] thiazole Derivatives and their Antiproliferative Activity against Melanoma Cell Line  

Park, Jin-Hun (Biomaterials Center, Korea Institute of Science and Technology)
Oh, Chang-Hyun (Biomaterials Center, Korea Institute of Science and Technology)
Publication Information
Bulletin of the Korean Chemical Society / v.31, no.10, 2010 , pp. 2854-2860 More about this Journal
Abstract
Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).
Keywords
Antiproliferative activity; Imidazo[2,1-b]thiazole; Cyclic sulfamide; A375; Melanoma;
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