[Synthesis and anti-tumor activities of 1,4-bis[3-(amino-dithiocarboxy)propionyl] piperazine derivatives].
OBJECTIVE
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 mumol.L-1. However, the inhibition of the other kinds of anti-tumor cells are not distinctive.


CONCLUSIONS
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.
Guo
B G
BG
School of Pharmaceutical Sciences, Beijing University, Beijing 100083, China.
Ge
Z M
ZM
Cheng
T M
TM
Li
R T
RT
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018922:HL-60 Cells / Q000187:drug effects; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D010879:Piperazines