Design, Synthesis And Anticancer Activity Of 1, 3-2H-1, 3-2O-2H-Isoindole-N-Substituted Derivates

Thalidomide was an old medicine that was withdrawn from widespread clinical use in the early 1960s because of its severe teratogenicity. But it is now in research as an inhibitor of angiogenesis in anticancer, anti-inflammatory effect, immunomodulatory effects and so on. In our reach, twenty three compounds 1,3-dihydro-1,3-dioxo-2H-isoindole thalidomide derivates were synthesized to find that whether they have anticancer activity. All the title compounds were identified by means of 1H-NMR, parts of them were identified by IR, MS.To test anticancer activity in vitro of the target compounds, cultured 4T1 cells (a kind of breast cancer cell) with medium buffer (10% New Calf Serum and 1% penicillin in DMEM) into 96-well plates, one day after, added drugs as designed. Following 72 hours after drug addition, performed an SRB test. The stained cells were then measured under a wavelength of 492 nm and the percent survival was calculated for each condition.The results of preliminary anticancer test showed that all title compounds exhibited potent anticancer activities to a certain extent. Anticancer activities of some target compounds were superior to that of thalidomide. The structure-activity relationship of the target compounds was also discussed, which will be good for further study of looking for novel anticancer drugs.