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A series of N-1 and N-2 aryl tetrahydroindazolone derivatives was synthesized and evaluated anticancer activity.The yield of N-1 products was more than those of corresponding N-2 by microwave core-cyclization.Both of N-1 and N-2 aryl tetrahydroindazolone were subjected into biological assay against bone cancer,liver cancer,colon cancer and lung cancer.Structure-activity relationship was elucidated the N-1 aryl tetrahydroindazolone possessed more potential activity than those of corresponding N-2 derivatives.The introduction of oxime moiety at 4-position of N-1 aryl tetrahydroindazoles led to a loss of the cytotoxic activity.The N-1 aryl tetrahydroindazole was shown the dramatically shrank down tumor growth under i.p.treatment comparated with those of Cisplatin in vivo assay.