Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters.
A variety of 4-N atom substituted derivatives were synthesized and evaluated for their in vitro anticancer activities using 4-methylpiperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl ester 4 as lead compound. Among them, compound 6a without any substituent on 4-N atom (R(1) = H) was found to be the most active anticancer agent with IC(50) = 5.3 microM against HL-60 and IC(50) = 11.5 microM against Bel-7402, respectively. Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity.
Hou
Xueling
X
School of Pharmaceutical Sciences, Peking University, Beijing, China.
Ge
Zemei
Z
Wang
Tingmin
T
Guo
Wei
W
Cui
Jingrong
J
Cheng
Tieming
T
Lai
Chingshan
C
Li
Runtao
R
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004050:Ditiocarb / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004952:Esters; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical
D000970:Antineoplastic Agents; D004952:Esters; D004050:Ditiocarb