Cao Sheng-li, Jiang Yu-yang, Feng Yu-ping, Liu Shi-ying, Gao Hong-he, Zhang Mei, Wan Rong
Department of Chemistry, Capital Normal University, Beijing 100037, China.
Yao Xue Xue Bao. 2007 Jul;42(7):741-6.
A series of 4(3H)-quinazolinone derivatives bearing dithiocarbamate side chains have been synthesized through the reaction of 6-bromomethyl-2-methyl-4(3H)-quinazolinone with CS2 and various amines in the presence of anhydrous K3PO4, and their structures were confirmed with ESI-MS, H NMR, elemental analysis or HRMS. The target compounds 8a -8q were tested for their in vitro antitumor activity against human myelogenous leukaemia K562 and human Hela cell lines by means of colorimetric MTT assay. Among the tested compounds, 8q exhibited in vitro inhibitory activity against K562 and Hela cells with IC50 values of 0.5 and 12.0 micromol x L(-01), respectively. Therefore, compound 8q is worthy to be a lead compound for the design and synthesis of new antitumor agents.
通过6-溴甲基-2-甲基-4(3H)-喹唑啉酮与二硫化碳及各种胺在无水磷酸钾存在下反应,合成了一系列带有二硫代氨基甲酸盐侧链的4(3H)-喹唑啉酮衍生物,其结构通过电喷雾电离质谱(ESI-MS)、氢核磁共振谱(H NMR)、元素分析或高分辨质谱(HRMS)得以确证。采用比色法MTT试验,对目标化合物8a - 8q针对人髓性白血病K562和人宫颈癌细胞系的体外抗肿瘤活性进行了测试。在所测试的化合物中,8q对K562和Hela细胞表现出体外抑制活性,其半数抑制浓度(IC50)值分别为0.5和12.0微摩尔/升。因此,化合物8q值得作为设计和合成新型抗肿瘤药物的先导化合物。