Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives

Abstract

In this paper, we described the synthesis of 2-aminothiazole sublibrary containing methyl, bromo, phenyl or butylidene at 4- or/and 5-position of its core. All target compounds were evaluated for their antitumor activities against human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compounds screened, 4,5,6,7-tetrahydrobenzo[d]thiazole(26b) exhibited the most potent antitumor activities with IC₅₀ values of 4.89 and 4.03 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated.

Keywords

2-Aminothiazole / Antitumor activity / Structure-activity relationship

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Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH