2,4-disubstituted thiazoles, part III - Synthesis and antitumor activity of ethyl 2-substituted-aminothiazole-4-carboxylate analogs

The synthesis of several new ethyl 2-substituted-aminothiazole-4-carboxylat e analogs is described. The prepared compounds were tested for their in vit ro antitumor activity against 60 human tumor cell lines by the National Can cer Institute (NCI) and showed potential anticancer activity. Ethyl 2-[3-(d iethylamino)propanamido]-thiazole-4-carboxylate (14) exhibited remarkable a ctivity against RPMI-8226 leukemia cell line with GI(50) value of 0.08 mu M , and a broad spectrum activity against all the tumor cell lines used with GI(50) (MG-MID) value of 38.3 mu M. The detailed synthesis and antitumor sc reening data are reported.