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目的:对金雀异黄素进行结构改造,合成5-羟基-4’-硝基-7-丙酰氧基异黄酮,并进行抗肿瘤活性研究。方法:以氯苄为起始原料,经氰基取代、硝化后,与间苯三酚经Friedel-Crafts反应和环合,再与丙酰氯发生酰化反应得到目标化合物,并采用MTT实验研究其体外抗肿瘤活性。结果:合成的目标化合物经熔点测定和1H-NMR确证其结构;目标化合物体外对人胃腺癌细胞株SGC-7901有较强的抑制活性。结论:金雀异黄素4’引入硝基,7位引入丙酰基后具有良好的抗肿瘤活性。
OBJECTIVE: To genotype genistein and synthesize 5-hydroxy-4’-nitro-7-propionyloxy isoflavone, and to study its antitumor activity. METHODS: Benzyl chloride was used as the starting material, which was substituted with cyano and nitrated. Friedel-Crafts reaction and cyclization with phloroglucinol followed by acylation with propionyl chloride gave the target compounds. MTT assay In vitro anti-tumor activity. Results: The target compound was confirmed by its melting point and 1H-NMR. The target compound showed strong inhibitory activity against human gastric adenocarcinoma cell line SGC-7901 in vitro. CONCLUSION: Genistein 4 ’can introduce nitro group and propionyl group 7 has good anti-tumor activity.