高等学校化学学报 ›› 2009, Vol. 30 ›› Issue (10): 1972.

• 研究论文 • 上一篇    下一篇

新型吲哚咔唑化合物的合成与抗肿瘤活性

江程1,2, 陈苏婷1,2, 尤启冬1,2, 李志裕1,2, 唐玮娟2   

  1. 1. 中国药科大学江苏省肿瘤发生与干预重点实验室,
    2. 药学院, 南京 210009
  • 收稿日期:2009-02-25 出版日期:2009-10-10 发布日期:2009-10-10
  • 通讯作者: 尤启冬, 男, 博士, 教授, 主要从事生物活性分子的设计与合成研究. E-mail: youqidong@gmail.com
  • 基金资助:

    江苏省自然科学基金(批准号: BK2005102)资助.

Synthesis and Bioactivities of Novel Indolocarbazole Derivatives

JIANG Cheng1,2, CHEN Su-Ting1,2, YOU Qi-Dong1,2*, LI Zhi-Yu1,2, TANG Wei-Juan2   

  1. 1. Jiangsu Key Laboratory of Carcinogenesis and Intervention,
    2. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
  • Received:2009-02-25 Online:2009-10-10 Published:2009-10-10
  • Contact: YOU Qi-Dong. E-mail: youqidong@gmail.com
  • Supported by:

    江苏省自然科学基金(批准号: BK2005102)资助.

摘要:

设计合成了一系列吲哚咔唑结构的抗肿瘤新化合物. 通过对反应溶剂进行选择和调整, 优化了吲哚咔唑母核合成的反应条件, 使后处理更为简便. 用溴化噻唑蓝四氮唑(MTT)法对所合成的9个目标化合物进行了体外细胞毒活性测试, 结果表明, 化合物4a, 4b, 4d, 4f和4i对人结肠癌HCT116和鼠白血病P388细胞的活性均强于阳性对照ED-571, 其中化合物4f对P388细胞的活性是阳性对照的10倍.

关键词: 吲哚咔唑; 抗肿瘤活性; 细胞毒活性

Abstract:

A series of novel indolocarbazole derivatives was designed and synthesized. The solvent was stu-died and the reaction conditions including solvent choice were optimized via easier operations. The cytotoxicities of the 9 target compounds were tested using MTT methods. The results indicate that compounds 4a, 4b, 4d, 4f and 4i show better in vitro activities against HCT116 and P388 than positive control ED-571 did. Particularly, compound 4f is 10 times more potential against P388 than ED-571.

Key words: Indolocarbazole; Anticancer activity; Cytotoxicity activity

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