有机化学 ›› 2010, Vol. 30 ›› Issue (07): 1084-087. 上一篇    下一篇

研究简报

4-苯基氨基喹唑啉衍生物的合成及体外抗白血病活性研究

刘鹰翔*1,张洋2,马玉卓2   

  1. (1广州中医药大学药物化学研究室 广州 510006)
    (2广东药学院药物化学系 广州 510006)
  • 收稿日期:2009-05-02 修回日期:2010-02-01 发布日期:2010-02-26
  • 通讯作者: 刘鹰翔 E-mail:liuyingxiang62@126.com
  • 基金资助:

    广东省自然科学基金(No. 04009620)资助项目

Synthesis of 4-Anilinoquinazoline and Evaluation of Its Antileukemic Activity

Liu Yingxiang*1 Zhang Yang2 Ma Yuzhuo2

  1. (1 Laboratory of Medicinal Chemistry, Guangzhou University of Chinese Medicine, Guangzhou 510006) (2 Department of Medicinal Chemistry, Guangdong Pharmaceutical University, Guangzhou 510006)
  • Received:2009-05-02 Revised:2010-02-01 Published:2010-02-26
  • Contact: LIU Ying-xiang E-mail:liuyingxiang62@126.com

为了寻找高效、低毒的抗白血病药物, 以JANEX-1为先导物, 设计并合成了8个未见文献报道的苯胺喹唑啉类化合物. 所有目标化合物的化学结构经IR, H NMR和元素分析确证. 体外抗人白血病K562细胞实验表明, 目标化合物的抗白血病活性高于JANEX-1.

关键词: 苯基氨基喹唑啉, 合成, 抗白血病

To search for more potent, less toxic anti-leukemic agents, eight new compounds using JANEX-1 as a lead have been designed and synthesized. Their structures were confirmed by IR, H NMR and elemental analyses. In addition, their in vitro antitumor activity against human leukemia cell line K562 shows that target compounds , and are more potent than JANEX-1.

Key words: anilinoquinazoline, synthesis, anti-leukemia