【摘要】 以3,5-二羟基苯甲酸为原料,分别经酯化、甲氧甲基保护或甲基化、酰肼化、氧化、醛酮缩合、脱保护基、O-法呢基化或O-异戊烯基化等步骤,以5.6%～46%的总收率合成了8个未见文献报道的查尔酮类化合物1a～1h,产物通过1HNMR,13CNMR,IR,MS进行了结构确证.对所合成的目标化合物在3个标准活性筛选模型中进行了生物活性试验,结果表明化合物1b在组织蛋白酶B(CAT-B)模型、化合物1e在细胞分离周期基因25表达的蛋白磷酸酶(CDC25)模型中表现出良好的活性.更多还原

【Abstract】 Eight novel chalcone compounds 1a～1h were synthesized by esterification, methoxymethyl protection or methylation, hydrazidation, oxidation, aldol condensation, deprotection, O-farnesylation or O-prenylation respectively using 3,5-dihydroxybenzoic acid as starting material in overall yields of 5.6%～ 46%. Their structures were confirmed by 1H NMR, 13C NMR, IR and MS spectra. Target compounds were screened with three international standard models for biological activity. Results showed that 1b against model CAT-B and 1e against model CDC25 possessed the good inhibition activity.更多还原