SYNTHESIS AND ANTI-TUMOR ACTIVITIES OF 1,4-BIS［3- (AMINO-DITHIOCARBOXY)PROPIONYL］ PIPERAZINE DERIVATIVES
- VernacularTitle: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
- Author:
Baoguo GUO
;
Zemei GE
;
Tieming CHENG
;
Runtao LI
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2001;36(3):185-187
- CountryChina
- Language:Chinese
-
Abstract:
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.
