Acta Chimica Sinica ›› 2011, Vol. 69 ›› Issue (04): 425-430. Previous Articles     Next Articles

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  1. (温州大学化学与材料工程学院 温州 325035)
  • 投稿日期:2010-08-31 修回日期:2010-09-26 发布日期:2010-10-11
  • 通讯作者: 胡茂林
  • 基金资助:


Synthesis and Biological Evaluation of Novel Coupling Derivatives of Photosensitizer and 5-fluorouracil as Antineoplastic Agents

LI Mei-Rong, CAI Xiao-Qing, ZHU Yi-Feng, LIU Kuan-Guan, HU Mao-Lin   

  1. (College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035)
  • Received:2010-08-31 Revised:2010-09-26 Published:2010-10-11
  • Contact: Mao-Lin Hu

Six novel conjugates of 5-fluorouracil photosensitizer for the photodynamic therapy research (PDT) were designed and synthesized. Their structures were characterized by 1H NMR, 13C NMR, IR and elemental analysis, 5-Fu and their octanol-water partition coefficients (lg P) were calculated by HPLC. Compounds 2a, 3a, 1b and 4b were evaluated by microculture tetrazolium assay (MTT) method for HL-60 cells and sulforhodamine B (SRB) method for BEL-7402 cells. The antitumor activities in vitro show that the compound 2a has a better inhibitory rate than 3a for both HL-60 and BEL-7402, as the octanol solubility of 2a is better than 3a. The compounds of 1b and 4b both show a moderate inhibiting effect, for the linkages of N—C is too stable to release 5-Fu.

Key words: 5-fluorouracil derivatives, photosensitizer agents, photodynamic therapy, octanol-water partition coefficients, anticarcinogenic activity