A series of thiazolo[5,4-]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activities against several human cancer cell lines. Structure-activity relationship studies were carried out, showing that most of the target compounds had good inhibition against the tested cell lines. Among them, compound exhibited potent inhibition against human gastric cancer cells MGC-803 and HGC-27 with IC values of 4.64 and 5.07 μM, respectively and around 12-fold selectivity between MGC-803 and GES-1, indicating a relatively low toxicity to normal cells. The potency and low toxicity of compound make the thiazolo[5,4-]pyrimidine an attractive scaffold for designing new derivatives selectively targeting MGC-803 cells.
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