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5-氟尿嘧啶-1-烷氧苯基三间氯苯基卟啉的合成及其体外抗癌活性

李雅1*,申利红1,王建森1,韩士田2   

  1. (1.河北邯郸学院化学系 邯郸 056005；2.河北师范大学化学与材料科学学院 石家庄 050016)
  • 收稿日期:2012-01-10 修回日期:2012-04-06 出版日期:2013-01-10 发布日期:2013-01-10
  • 通讯作者: 李雅，教授; Tel/Fax:0310-6260301; E-mail:liya1962@126.com; 研究方向：卟啉化合物的合成及性能
  • 基金资助:
    河北省科学技术研究与发展指令计划(09276418D-21)邯郸市科学技术研究与发展指令计划(1023108098-10)和邯郸学院博硕基金(2010011)资助项目

Synthesis and Antitumor Activity in Vitro of 5-Fluorouracil-1-alkylaxgphenyl-tetra m-Chlorophenyl Porphyrin Compounds

LI Ya1*, SHEN Lihong1, WANG Jiansen1, HAN Shitian2   

  1. (1.Department of Chemistry,Handan College,Handan 056005,China;
    2.College of Chemistry & Material Science,Hebei Normal University,Shijiazhuang 050016,China)
  • Received:2012-01-10 Revised:2012-04-06 Published:2013-01-10 Online:2013-01-10

PDF

1696

被引次数

3

摘要： 为提高5-氟尿嘧啶抗癌的靶向性,降低其不良反应,合成了5种新型卟啉-5-氟尿嘧啶衍生物及其Mn3+配合物,优化了合成反应条件,探索了目标化合物的分离方法。 通过IR、UV-Vis、1H NMR和ESI-MS对化合物结构和组成进行了确认。 采用四甲基偶氮唑蓝(MTT)比色法，以5-氟尿嘧啶为阳性对照药，测试了卟啉化合物对5种肿瘤细胞的体外抑制活性。 初筛结果显示，化合物D3对人卵巢癌细胞Sk-ov-3有较强的抑制作用。

关键词: 卟啉, 氟尿嘧啶, 合成, 体外抗癌活性

Abstract: To search for more potential antitumor agents, five new porphyrin-5-fluorouracil compounds were designed and synthesized. The reaction conditions were optimized and the separation method of the target products was explored. The compositions and structures of these compounds were confirmed by IR, UV-Vis, 1H NMR and MS. Their cytotoxicity against five human cancer cell lines in vitro was evaluated by MTT assay. Biological screening results demonstrate that some tested compounds exhibit potential antitumor activity, particularly, compound D3 shows more potential cytotoxic activities than the control 5-fluorouracil against Sk-ov-3 cells.

Key words: porphyrin, Fluorouraci, synthesis, antitumor activity in vitro

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