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Novel 2-aminoimidazolone derivatives were synthesized. Most compounds displayed strong anticancer activities against human carcinoma cells in vitro. Compounds 8a, 8b and 8j exhibited optimal activity superior to 5-FU in most cancer cells tested. Especially, the IC 50 s of 8b (12.6–21.5μmol/L) against five tumor cells were 1–4 fold less than those of 5-FU (18.4–56.1μmol/L) in vitro. Furthermore,...
Novel farnesylthiosalicylic acid (FTA) derivatives 5a–m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5c, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cells tested. Furthermore, 5e induced tumor cell apoptosis, which was accompanied by lower Bcl-2 expression, but with higher Bax and caspase 3 expression activities in cancer cells.
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