Synthesis and Antitumor Activities of Novel 4-Morpholinothieno [3,2-d]pyrimidine Derivatives

A series of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives was designed and synthesized. All of them were screened for their cytotoxic activities against large cell lung cancer(H460), colon cancer (HT-29) and adenocarcinomic lung cancer(A549) cell lines in vitro. The pharmacological results indicate that most of the target compounds show moderate to significant activities. Especially compound 17 exhibits the most potent antitumor activities against H460, HT-29 and A549 cell lines with IC₅₀ values of 0.57, 0.45 and 1.45 μmol/L, respectively.