DESIGN, SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY EVALUATION OF NEW 5-AZAISOINDIGO DERIVATIVES

摘要

New 5-azaisoindigo derivatives were synthesized with two key intermediates 5-azaoxindole (7) and substituted indole-2,3-dione (10) in this paper. Intermediate 7 was prepared from 3-methylpyridine (1) through 6 steps containing oxidation reaction and so on. Intermediate 10 was obtained by a convenient Sandmeyer's method. The target compounds 5-azaisoindigo derivatives lla-f were obtained by condensation of these two intermediates 7 and 10 in acidic condition. All target compounds were evaluated for their antiproliferative activity against seven cell lines by SRB assay. Compounds lie and llf showed significant antiproliferative activity against K562 cells (IC50: 8.9 uM and 13.6 uM, respectively).