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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 31, Number 10
BKCSDE 31(10)
October 20, 2010 

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
Jin Hun Park, Chang Hyun Oh*
Antiproliferative activity, Imidazo[2,1-b]thiazole, Cyclic sulfamide, A375, Melanoma
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 (IC50 = 1.9 μM) also demonstrated more potent antiproliferative activity compared with Sorafenib (IC50 = 5.6 μM).
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