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Five bioactive dehydroabietylamine Schiff-base derivatives ( L 1 -L 5 ) had been synthesized from Dehydroabietylamine ( L 0 ), and the complex Cu(L 1 ) 2 had been obtained from the compound L 1 and copper(II) acetate. Their activities against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver) and HUVEC (umbilical vein, normal cell) in vitro were investigated. The toxicity of L 1 -L 5 and Cu(L 1 ) 2 was all lower than L 0 . For MCF-7 cell, L 1 , L 3 , L 4 , L 5 and Cu(L 1 ) 2 had higher antitumor activity than L 0 . The smallest IC 50 value was 2.58  μ M of L 5 . For A549 cell, the IC 50 value of the compound L 4 was smaller than L 0 , which indicated that the compound L 4 had higher anti-A549 activity than L 0 . For HepG2 cell, the IC 50 value of L 4 ( 0.24  μ M) and L 5 (0.14  μ M) were much smaller than L 0 , which suggested L 4 and L 5 had higher anti-HepG2 activity. L 5 was 180 times more effective at inhibiting cultured HepG2 cells survival than normal cells, with average IC 50 values of 0.14 and 25.56  μ M. Furthermore, L 0 , L 4 and L 5 contrasting with Doxorubicin had been measured with the ability to induce apoptosis. It turned out that L 4 and L 5 could induce more HepG2 cells apoptosis, which suggested they may be potential antitumor drugs. [ABSTRACT FROM AUTHOR]