高等学校化学学报2016，Vol.37Issue(6)：1093-1099,7.DOI:10.7503/cjcu20160103
双-β-咔啉衍生物的设计、合成及抗肿瘤活性
Design, Synthesis and in vitro Antitumor Activities of Novel Bivalent β-Carbolines
摘要
Abstract
A series of novel bivalent β-carbolines with a spacer of three to ten methylene units between the 7-oxygen was synthesized and characterized by nuclear magnetic resonance ( NMR ) and mass spectrometry (MS). The antitumor activities against Bel-7402, 786-0, BGC-823, A375, 769-P and MCF7 cell lines in vitro were investigated by MTT method. The results demonstrated that compounds 4c, 4k and 4r were almost inactive against all tumor cell lines, compounds 4g and 4o displayed significant cytotoxic activities with IC50 value of lower than 10μmol/L against all tumor cell lines. Most compounds displayed good and selective cyto-toxic activities against HT-29 and Blu-87 cell lines. Primary structure-activity relationships( SARs) analysis indicated that the length of the spacer affected cytotoxic activities in vitro, and 8—10 methylene units were more favorable. Moreover, n-butyl or i-butyl substituents in position-9 of β-carboline facilitated the antitumor potencies.关键词
去氢骆驼蓬碱/β-咔啉/抗肿瘤活性/构效关系Key words
Harmine/β-Carboline/Antitumor activity/Structure-activity relationship分类
化学化工引用本文复制引用
郭亮,曹日晖,范文玺,甘紫云,马芹..双-β-咔啉衍生物的设计、合成及抗肿瘤活性[J].高等学校化学学报,2016,37(6):1093-1099,7.基金项目
新疆生产建设兵团中青年科技创新领军人才计划项目(批准号:2015BC001)资助 （批准号:2015BC001）
