SYNTHESIS AND ANTI-TUMOR ACTIVITIES OF 1,4-BIS[3- (AMINO-DITHIOCARBOXY)PROPIONYL] PIPERAZINE DERIVATIVES / 药学学报
Acta Pharmaceutica Sinica
; (12): 185-187, 2001.
Article
en Zh
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| ID: wpr-410887
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WPRO
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.
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Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2001
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Article