β-咔啉环取代脲类Raf激酶抑制剂的设计、合成及生物活性研究
esign, Synthesis and Biological Evaluation of β-Carboline-substituted Urea Derivatives as Novel Potent Raf Kinase Inhibitors
目的 设计合成β-咔啉环取代的脲类化合物，体外筛选其对人结肠癌细胞HT-29及人肝癌细胞SMMC-7721的抑制活性，研究构效关系。方法 经过环合、酯化、脱氢等反应合成目标化合物，采用MTT法测定目标化合物抑制HT-29与SMMC-7721的活性。结果合成了14个未见文献报道的化合物，结构经红外光谱、核磁共振氢谱、质谱确证。结论目标化合物I-6和I-7对SMMC-7721有中效的抑制活性，而对照药索拉菲尼有基本没有抑制活性，有望成为先导物，进行进一步的研究。
im To design and synthesize novel of β-carboline-substituted urea derivatives. Evaluate their inhibitory activities against HT-29 cell and SMMC-7721 cell. Methods The 14 target compounds were synthesized through cyclization, esterification, dehydrogenation, nitration reactions, etc. and their inhibitory activities were assayed in vitro. Results 14 target compounds were prepared which have not been reported in literatures. Their structures were characterized by IR, 1H-HMR and MS. Conclusion Compound I-6 and I-7 demonstrated potent SMMC-7721 inhibitory activities as compared with the positive control Sorafenib, which may provide a promising lead for further structure optimizations.
唐伟方、辛波涛、陆涛、宋艳、周娟、陈亚东
药学基础医学生物化学
药物化学Raf激酶抑制剂抗肿瘤合成
medicinal chemistryRaf kinase inhibitorsantitumorsynthesis
唐伟方,辛波涛,陆涛,宋艳,周娟,陈亚东.β-咔啉环取代脲类Raf激酶抑制剂的设计、合成及生物活性研究[EB/OL].(2012-02-16)[2025-05-06].http://www.paper.edu.cn/releasepaper/content/201202-539.点此复制
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