Syntheses and Antitumor Activities of Phenylpiperazine Derivatives

Abstract

The structure of phenylpiperazine as an important pharmacophore could generate wide pharmacological activities. In this work,a series of novel phenylpiperazine derivatives was designed,synthesized and their preliminary antiproliferative activities against tumor cell lines were evaluated using MTT assay. Results indicated that the most active target compound 4t had the substitution of benzenesulfonamides and benzofuran on N1 and N4 position of piperazine respectively. Furthermore,IC_(50) values of compound 4t against five tumor cell lines in vitro were determined. Compound 4t could inhibit the growth of some tumor cell lines and showed similar inhibitory activities against MDA-MB-231 tumor cell line( IC_(50)= 3. 50 μmol/L) compared with Gossypol( IC_(50)= 1. 40 μmol/L). These results provided useful information for designing new phenylpiperazine derivatives with higher antitumor activity.