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

Bulletin of the Korean chemical society

Jin Hun Park¹  Chang Hyun Oh¹ 

关键词: Antiproliferative activity;    Imidazo[2;    1-b]thiazole;    Cyclic sulfamide;    A375;    Melanoma;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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 レM) also demonstrated more potent antiproliferative activity compared with Sorafenib (IC₅₀ = 5.6 レM).

【 授权许可】

Unknown