Fifteen novel 2-methyl-3-(1',2'-O-cyclohexylidendioxyethyl)-5-aryl-3a,6a-dihydro-4,6-dioxopyrrolino[3',4'-d]- isoxazolinium-tetrachloroferrate derivatives 4a～4o were synthesized by N-methylation of the corresponding isoxazoline using dimethyl sulfate as a methylating reagent and ferric(III)-chloride as anion exchange reagent in hydrochloric acid. The structures of the target compounds 4a～4o were characterized by ¹H NMR, IR spectra and elemental analysis. The preliminary in vitro bioassay on the compounds showed that most compounds possess anti-cancer activity and the Leukocyte common antigen activity at some extent. At the test concentration of 20 μg/mL, all compounds showed inhibition activity of ≥97.55% against Cdc25B (cell division cycle 25B) phosphatase except for compound 4h, and inhibition activity of 68.41%～93.38% against leukocyte common antigen (LCK) CD45 protein tyrosine phosphatase A, respectively. Preliminary discussion was carried out on the structure-activity relationship of the target compounds.

Key words: N-methylisoxazolinium-tetrachloroferrate, synthesis, bioactivity