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.
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Supported by the Science and Technology Development Project of Shandong Province, China(No.2012GSF11812), the Natural Science Foundation of Shandong Province, China(No.ZR2015BL006) and the Project of Shandong Province Higher Educational Science and Technology Program, China(No.J15LM08).
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Li, H., Wang, X., Duan, G. et al. Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives. Chem. Res. Chin. Univ. 32, 929–937 (2016). https://doi.org/10.1007/s40242-016-6304-2
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DOI: https://doi.org/10.1007/s40242-016-6304-2