6-(Methoxyphenyl)tetrahydroindazol-4-one derivatives were synthesized and evaluated for antiproliferative activity. Structure-activity relationship was elucidated with various substitutions on the N-l aryl moiety of tetrahydroindazol-4-one. A novel N-2 aryl-substituted skeleton was established by microwave synthesis. The bioevaluative result was shown that the N-\ substituted tetrahydroindazol-4-one possessed more potential activity against human lung cancer cell (H226), leukemia (Jurkat cell), and nasopharyngeal carcinoma cell (NPC-TW01) in vitro than those of corresponding N-2 derivatives. The introduction of oxime moiety at 4-position of tetranyaroinaazoiones iea to a loss 01 me cyioiuAiactivity.
