5-氟尿嘧啶修饰卟啉的合成及抗肿瘤活性

摘要

合成了一种5-氟尿嘧啶修饰的自由卟啉（5-[2-（5-氟尿嘧啶-3-基）乙氧基苯基]-10，15，20-三（4-甲氧基苯基）卟啉）及其2种金属卟啉配合物：5-[2-（5-氟尿嘧啶-3-基）乙氧基苯基]-10，15，20-三（4-甲氧基苯基）锰卟啉和5-[2-（5-氟尿嘧啶-3-基）乙氧基苯基]-10，15，20-三（4-甲氧基苯基）锌卟啉。通过紫外可见光谱（UV-Vis）、红外光谱（IR）和核磁共振谱氢谱（1 H NMR）对目标化合物进行了结构表征。用噻唑蓝法（MTT法）测定了自由卟啉、锰卟啉及锌卟啉分别对肺腺癌细胞株A549、肝癌细胞株Bel7402和人结肠癌细胞株HCT-8的抑制活性。其中，锰卟啉对人结肠癌细胞株HCT-8的半抑制浓度为IC50为17.8 mg／L，具有一定的细胞毒作用。%The porphyrin modified with 5-fluorouracil(5-[2-(5-fluorouracil-3-yl)-ethoxyphenyl]-10,15,20-tri ( 4-methoxyphenyl ) porphyrin ) and its two metal porphyrin complexes: 5-[ 2-( 5-fluorouracil-3-yl )-ethoxyphenyl]-10,15,20-tri(4-methoxyphenyl) Mn porphyrin and 5-[2-(5-fluorouracil-3-yl)-ethoxyphenyl]-10,15,20-tri(4-methoxyphenyl ) Zn porphyrin were synthesized .The structures of the three compounds were characterized by ultraviolet visible spectroscopy ( UV-Vis ) , infred spectroscopy ( IR ) and proton nuclear magnetic resonance spectroscopy(1H NMR).The antitumor activities of these compounds to A549, Bel7402, HCT-8 were tested using the methyl thiazolyl tetrazolium ( MTT) method.The results show that the IC 50 value of Mn porphyrin to HCT-8 is 17.8 mg/L.