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To explore novel antitumor agents with high efficiency and low toxicity, riluzole alkyl derivatives (4a-4i) were synthesized. Their anti-proliferative activities against HeLa, HepG2, SP2/0, and MCF-7 cancer cell lines were assessed by the CCK-8 assay and compared with human normal liver (LO2) cells. Most of them showed potent cytotoxic effects against four human tumor cell lines and low toxic to LO2 cells. In particular, 2-(N-ethylamine)-6-trifluoromethoxy- benzothiazole (4a) showed a IC50 value of 7.76 μmol/L in HeLa cells and was found to be nontoxic to LO2 cells up to 65 μmol/L. Furthermore, flow cytometry indicated that 4a could induce remarkable early apoptosis and G2/M cell cycle arrest in HeLa cells. It also impaired the migration ability of HeLa cells in wound healing assays. Western blot results demonstrated that 4a suppressed Bcl-2 protein expression but increased the level of Bax in HeLa cells, and elevated the Bax/Bcl-2 expression ratio. These new findings suggest that 4a exhibited beneficially anti-cervical cancer effect on HeLa cells by inducing HeLa cell apoptosis.

The calculation of order parameteres with variant temperature in Ll2 structure has been carried out in this work by means of Monte Carlo method statistical physics. The order interaction of the nearest neighbour J1 and three kinds of order interaction of next neares' neighbour J2= 0, - 0.3J1 as well as 0.3J1 were considered in this calculation. The results show that the calculation value of the critical temperature Tc (order-disorder transition temperature) of the first order phase transformation is in good agreement with that obtained by some other theories, such as quasi-chemical method; and Tc is sensitively affected by J2, that may be regarded as an interpretation about the action of interstitial atoms in Ll2 structure.