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间氯苯基锰卟啉-5-氟尿嘧啶配合物的合成及其对癌细胞的抑制活性

韩军兴,刘彦钦*,韩士田   

  1. (河北师范大学化学与材料科学学院 石家庄 050024)
  • 收稿日期:2011-08-15 修回日期:2011-10-21 出版日期:2012-06-10 发布日期:2012-06-10
  • 通讯作者: 刘彦钦，教授; Tel/Fax:0311-80787400; E-mail:liuyq2002@163.com; 研究方向：有机合成
  • 基金资助:
    河北省自然科学基金(203147)资助项目

Synthesis of m-Chlorophenyl Mn-Porphyrin-5-Fluorouracil Complexes and Their Inhibition Activity to Cancer Cells

HAN Junxing, LIU Yanqin*, HAN Shitian   

  1. (College of Chemistry and Material Science,Hebei Normal University,Shijiazhuang 050024,China)
  • Received:2011-08-15 Revised:2011-10-21 Published:2012-06-10 Online:2012-06-10

PDF

1099

被引次数

2

摘要： 合成了4种新5-氟尿嘧啶-卟啉衍生物：5-[3-(2-(5-氟尿嘧啶-1-基)乙氧基)苯基]-10,15,20-三(3-氯苯基)卟啉(1a)、5-[3-(2-(5-氟尿嘧啶-1-基)乙氧基)苯基]-10,15,20-三(3-氯苯基)锰卟啉(2a)、5-[3-(3-(5-氟尿嘧啶-1-基)丙氧基)苯基]-10,15,20-三(3-氯苯基)锰卟啉(2b)和5-[3-(4-(5-氟尿嘧啶-1-基)丁氧基)苯基]-10,15,20-三(3-氯苯基)锰卟啉(2c)，通过UV-Vis、IR、MS及元素分析表征了它们的结构。 用噻唑蓝法（MTT法）测定了化合物2a、2b和2c对人胃癌细胞株BGC-823的抑制活性。 化合物2b的半数抑制浓度IC50为1.34 μmol/L，表明有一定的细胞毒作用。

关键词: 锰卟啉, 氟尿嘧啶, 合成, 人胃癌细胞株BGC-823

Abstract: Four porphyrin-5-fluorouracil conjugates, i.e. 5-[3-(2-(5-fluorouracil-1-yl)-ethoxy)phenyl]-10,15,20-tri(3-chlorophenyl)porphyrin(1a), 5-[3-(2-(5-fluorouracil-1-yl)-ethoxy)phenyl]-10,15,20-tri(3-chlorophenyl)Mn-porphyrin(2a), 5-[3-(3-(5-fluorouracil-1-yl)-propoxy)phenyl]-10,15,20-tri(3-chlorophenyl)Mn-porphyrin(2b) and 5-[3-(4-(5-fluorouracil-1-yl)-butoxy)phenyl]-10,15,20-tri(3-chlorophenyl)Mn-porphyrin(2c), were successfully synthesized and characterized by UV-Vis, IR, MS and elemental analysis. Inhibition activity of the synthesized compounds(2a, 2b and 2c) to human gastric cancer cell line BGC-823 was tested using the methyl thiazolyl tetrazolium(MTT) method. The IC50 value of 2b was 1.34 μmol/L, indicating that compound 2b had certain cytotoxic effect.

Key words: manganoporphyrin, fluorouracil, synthesis, human gastric cancer cell line BGC-823

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