| Summary: | Three series of novel thienopyrimidine derivatives <b>9a</b>−<b>l</b>, <b>15a</b>−<b>l</b>, and <b>18a</b>−<b>h</b> were designed and synthesized, and their IC<sub>50</sub> values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound <b>9a</b> showed moderate activity with IC<sub>50</sub> values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 µM, respectively. The inhibitory activities of compounds <b>9a</b> and <b>15a</b> against PI3Kα and mTOR kinase were further evaluated. Compound <b>9a</b> exhibited PI3Kα kinase inhibitory activity with IC<sub>50</sub> of 9.47 ± 0.63 µM. In addition, docking studies of compounds <b>9a</b> and <b>15a</b> were also investigated.
|
|---|