Abstract:

Recently, more and more thiazole compounds were reported to exhibit antitumor activities. Twenty-nine new 5-benzyl-4-tert-butyl-N-arylthiazol-2-amine hydrobromides were synthesized from arylamino and 2-bromo-4,4-dimethyl-1-arylpentan-3-one. Their structures were confirmed by ¹H NMR spectra and elemental analysis. The data of antitomor activities in vitro indicated that the IC₅₀ values of compounds A4, A5, A12 and A29 against A549 cells were 0.016, 0.019, 0.019 and 0.026 μmol/mL, respectively, similar to Taxinol(IC₅₀value was 0.022 μmol/mL). The IC₅₀ values of compounds A5, A7, A13, A14 and A19 against Bel7402 were 0.021, 0.021, 0.026, 0.014 and 0.029 μmol/mL, respectively, similar to Taxinol(IC₅₀ value was 0.030 μmol/mL). The shape changes of A549 cells were observed by inverted microscope and flourescence microscope after staining with Hoechst 33342-PI.

Key words: 5-Benzyl-4-tert-butyl-N-arylthiazol-2-amine hydrobromide, Synthesis, Antitumor activity