Liu Jianzhen, Liang Wen, Wang Yuanyou, Zhao Guisen
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong, China.
Drug Discov Ther. 2013 Aug;7(4):144-52.
A new series of anthranilamide derivatives were synthesized and evaluated for their antiproliferative activities against human colon carcinoma cell lines (HCT 116) and human breast adenocarcinoma cell lines (MDA-MB-231) in vitro. The bioassay results indicated that compounds 7a-7d, 11a, and 11b with flexible linkers showed promising antiproliferative activity against both cell lines. Among the compounds synthesized, 7c showed the most significant antiproliferative activity. Flow cytometric analysis indicated that 7c inhibited HCT 116 and MDA-MB-231 cell growth by inducing apoptosis in a dose-dependent manner and suppressed HCT 116 cell proliferation by G1 and S phase arrest. Compound 7c may serve as a lead candidate in the development of novel anticancer agents.
合成了一系列新的邻氨基苯甲酰胺衍生物，并在体外评估了它们对人结肠癌细胞系（HCT 116）和人乳腺腺癌细胞系（MDA-MB-231）的抗增殖活性。生物测定结果表明，具有柔性连接基团的化合物7a - 7d、11a和11b对这两种细胞系均显示出有前景的抗增殖活性。在合成的化合物中，7c表现出最显著的抗增殖活性。流式细胞术分析表明，7c通过剂量依赖性诱导凋亡抑制HCT 116和MDA-MB-231细胞生长，并通过G1期和S期阻滞抑制HCT 116细胞增殖。化合物7c可能作为新型抗癌药物开发的先导候选物。
