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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

Title	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
Author	Jin Hun Park, Chang Hyun Oh*
Keywords	Antiproliferative activity, Imidazo[2,1-b]thiazole, Cyclic sulfamide, A375, Melanoma
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 (IC₅₀ = 1.9 μM) also demonstrated more potent antiproliferative activity compared with Sorafenib (IC₅₀ = 5.6 μM).
Page	2854 - 2860
Full Text	PDF

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