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Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive a-aminophosphonate subunits were introduced at the N3 position through an N–N bond connection.The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells(EC109), human hepatocarcinoma cells(Hep G2), human gastric carcinoma cells(MGC-803),respectively, by the MTT method. The evaluation results revealed that compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted the most potent inhibition against Hep G2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against Hep G2(91.2%) and MGC-803(94.4%) cells.
Two series of thieno [2,3-d] pyrimidine derivatives were designed and synthesized, in which bioactive a-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested The human liver carcinoma cells (Hep G2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that these compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted The most potent inhibition against Hep G2, MGC-803 and EC109 cells, respectively, 6 mg of presented inhibitory effect against Hep G2 (91.2%) and MGC-803 (94.4%) cells.