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Acta Chimica Sinica ›› 2011, Vol. 69 ›› Issue (04): 425-430. Previous Articles Next Articles
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李美容,蔡晓庆*,朱易峰,刘宽冠,胡茂林*
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国家自然科学基金项目;浙江省教育厅自然科学基金
LI Mei-Rong, CAI Xiao-Qing, ZHU Yi-Feng, LIU Kuan-Guan, HU Mao-Lin
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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
LI Mei-Rong, CAI Xiao-Qing, ZHU Yi-Feng, LIU Kuan-Guan, HU Mao-Lin. Synthesis and Biological Evaluation of Novel Coupling Derivatives of Photosensitizer and 5-fluorouracil as Antineoplastic Agents[J]. Acta Chimica Sinica, 2011, 69(04): 425-430.
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