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ID: ALA1146850

Journal: Bioorg Med Chem Lett

Title: Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters.

Authors: Hou X, Ge Z, Wang T, Guo W, Cui J, Cheng T, Lai C, Li R.

Abstract: 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.

CiteXplore: 16766185

DOI: 10.1016/j.bmcl.2006.05.085