【摘 要】
：
以2,4-二氨基-6-羟甲基吡啶并[3,2-d]嘧啶为原料,与对甲酰基苯甲酰谷氨酸二乙酯发生Wittig反应构建叶酸类似物的骨架结构,还原吡啶环得到4-氨基-8,10-二碳杂四氢叶酸类似物,
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以2,4-二氨基-6-羟甲基吡啶并[3,2-d]嘧啶为原料,与对甲酰基苯甲酰谷氨酸二乙酯发生Wittig反应构建叶酸类似物的骨架结构,还原吡啶环得到4-氨基-8,10-二碳杂四氢叶酸类似物,在N5位取代不同基团得到四个新的4-氨基-N8,N10-二碳杂四氢叶酸类化合物,经1H NMR,13C NMR和MS对化合物的结构进行了表征.初步生物活性结果表明,此类化合物对人重组胸苷酸合成酶的抑制作用与N5位取代基有关,2个化合物在0.1μmol L-1的浓度下对HL-60白血病细胞的抑制率达到60%以上.
Wittig reaction of 2,4-diamino-6-hydroxymethylpyrido [3,2-d] pyrimidine with diethyl p-formylbenzoyl glutamate to construct the structure of folic acid analogues, Reduction of the pyridine ring to give 4-amino-8,10-dicarbotetrahydrofolate analogs, in the N5 position to replace different groups to give four new 4-amino-N8, N10-dicarbonate tetrahydrofolate compounds, The structures of the compounds were characterized by 1H NMR, 13C NMR and MS.The preliminary bioassay results showed that the inhibitory effect of these compounds on human recombinant thymidylate synthase was related to the N5 substituent, -1 concentration of HL-60 leukemia cells in the rate of more than 60%.
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