Design, synthesis, and biological evaluation of new thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents

Abstract

A series of thiazolo[5,4-<i>d</i>]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 <b>7i</b> exhibited potent inhibition against human gastric cancer cells MGC-803 and HGC-27 with IC₅₀ 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 <b>7i</b> make the thiazolo[5,4-<i>d</i>]pyrimidine an attractive scaffold for designing new derivatives selectively targeting MGC-803 cells.