【摘要】 合成了一系列结构全新的苯基哌嗪类衍生物,采用溴化噻唑蓝四氮唑(MTT)法进行了初步体外抗肿瘤细胞增殖活性研究.结果表明,当哌嗪环4位连有苯磺酰胺结构时,其1位引入苯并呋喃结构的目标化合物4t的活性最好.化合物4t对多种瘤株具有明显抑制作用,特别是对人乳腺癌细胞MDA-MB-231的增殖抑制强度与阳性对照药棉酚相近.更多还原

【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,IC₅₀ 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( IC₅₀= 3. 50 μmol/L) compared with Gossypol( IC₅₀= 1. 40 μmol/L). These results provided useful information for designing new phenylpiperazine derivatives with higher antitumor activity.更多还原