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设计合成了六种新型的适用于新一代肿瘤治疗法——光动力学疗法研究的5-氟尿嘧啶(5-Fu)光敏性偶联衍生物.目标化合物的结构经过1H NMR,13C NMR,IR和元素分析确证,并通过HPLC法测定了它们及5-Fu的表观油水分配系数.其中四种化合物2a,3a,1b和4b分别采用四氮唑盐法(MTT法)对白血病细胞株HL-60和磺酰罗丹明B蛋白染色法(SRB法)对肝癌细胞株BEL-7402进行了体外抗癌活性测试.结果表明,噻吩一取代产物2a的表观油水分配系数大于二取代产物3a,与生物活性测试结果表明的2a和3a对HL-60和BEL-7402的抑制率呈正相关性;而由于N—C键过于稳定不易断裂,导致两种硝基苄基衍生物1b和4b对HL-60和BEL-7402的抑制率都比较低.
Six novel 5-fluorouracil (5-Fu) photosensitized derivatives suitable for the next generation of tumor therapy, photodynamic therapy, were designed and synthesized.The structures of target compounds were characterized by 1H NMR, 13C NMR, IR and Elemental analysis confirmed that the apparent oil-water partition coefficients of 5-Fu and 5-Fu were determined by HPLC.The four compounds 2a, 3a, 1b and 4b were respectively treated with MTT method to detect the leukemia cell line HL- 60 and Sulforhodamine B protein staining (SRB method) were used to test the anticancer activity of hepatoma cell line BEL-7402 in vitro.The results showed that the apparent oil-water partition coefficient of thiophene-substituted product 2a was larger than that of disubstituted product 3a and The bioassay results showed that 2a and 3a showed a positive correlation between the inhibitory rates of HL-60 and BEL-7402. However, the stability of the two nitrobenzyl derivatives 1b and 4b to HL- 60 and BEL-7402 have lower inhibition rates.