Synthesis And Anticancer Activity Of New Spirooxindoles Incorporating[1,2,4]Triazolo[3,4-B][1,3,4]Thiadiazine Moiety

A series of new spirooxindole derivatives (4a-41) were designed, synthesized and characterized, in which the structure of compound 4f was further confirmed by single X-ray diffraction.Their antiproliferative activities were evaluated in vitro by MIT assay, the results indicated that most of the prepared compounds exhibited moderate to potent antiproliferative activities against four cancer cell lines, DU145, EC109, MGC803, and MCF-7. Particularly, compound 4d showed 3.0, 1.6, 2.7 and 1.3 times more active than positive control 5-fluorouracil (IC50 = 24.29 +/- 0.04 mu M, 10.38 +/- 0.01 mu M, 25.54 +/- 0.05 mu M, 22.46 +/- 0.03 mu M) in inhibiting DU145, EC109, MGC803, and MCF-7 cell proliferation with IC50 values of 8.02 +/- 0.64 mu M, 6.62 +/- 0.89 mu M, 9.49 +/- 0.78 mu M, and 17.65 +/- 0.82 mu M, respectively. These encouraging results should provide important information for the development of new anticancer agents. (C) 2020 Published by Elsevier B.V.