1,4-二[3-(氨基硫代甲酰硫基)丙酰基]哌嗪类化合物的合成及其抗肿瘤活性

SYNTHESIS AND ANTI-TUMOR ACTIVITIES OF 1,4 BIS[3- (AMINO-DITHIOCARBOXY)PROPIONYL] PIPERAZINE DERIVATIVES

目的 寻找并合成低毒、有较强抗肿瘤活性的哌嗪类化合物。方法和结果 以 1,4 二 (3 溴丙酰基 )哌嗪为先导物 ,合成了一系列 1,4 二 [3 (氨基硫代甲酰硫基 )丙酰基 ]哌嗪类新化合物 ,并测试了这些化合物 (4a - j)对 8种瘤细胞株的体外抗肿瘤活性。结论 体外抗肿瘤活性试验结果表明 ,大多数化合物显示一定的抗肿瘤活性 ,尤其是化合物 4c,4d和 4e,浓度在 10 μmol·L-1时 ,对HL 6 0细胞抑制率分别为 44 % ,90 %和 70 %。

AIM To synthesize piperazine derivatives and screen anti tumor compounds with higher activity and lower toxicity. METHODS Selecting 1,4 bis(3 bromopropionyl)piperazine as leading compound, a series of 1,4 bis[3 (amino dithiocarboxy)propionyl] piperazine derivatives (4a-j) were synthesized through the use of aminodithiocarboxylate. All the synthetic compounds (4a-j) were tested for their anti tumor activity against eight kinds of tumor cells. RESULTS Compounds (4a-j) are new compounds, among them, compounds 4c, 4d and 4e showed anti tumor activity against HL 60. The inhibition of compounds 4c, 4d and 4e against HL 60 are 44%, 90% and 70% respectively, at the concentration of 10 μmol·L -1 . However, the inhibition of the other kinds of anti tumor cells are not distinctive. CONCLUSION These results suggest that this may be one of the effective routes to improve the anti tumor activity and reduce the toxicity of 1,4 bis(3 bromopropionyl)piperazine.