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以间苯二酚和对苯二酚为起始原料,经过傅克酰化、Baker-Venkataraman重排、关环三步反应分别得到5个7-羟基黄酮和5个6-羟基黄酮类化合物.试验结果发现,这些化合物溶解性能不好,生物活性不高,因此,对这些化合物又经过苯甲酰化并将7-羟基黄酮与1-氯-3-溴丙烷首先发生亲核取代反应,然后和诺氟沙星在丙酮中反应生成化合物13,总共得到了5个结构新颖的黄酮和4个未见文献报道的β-丙二酮类化合物.通过四甲基偶氮唑盐(MTT)法对19个化合物的抑制人宫颈癌细胞Hela活性进行了体外评价,结果表明:化合物13的半数抑制浓度IC50为19.4μmol/L,具有深入研究的价值.
Using resorcinol and hydroquinone as starting materials, five 7-hydroxyflavone and five 6-hydroxyflavonoids were obtained through Frieff acylation, Baker-Venkataraman rearrangement and ring-closing reaction. The experimental results showed that these compounds were poorly soluble and had low biological activity. Thus, these compounds were benzoylated and reacted with nucleophilic substitution of 7-hydroxyflavone and 1-chloro-3-bromopropane first, and then And norfloxacin were reacted in acetone to give compound 13. A total of five novel flavonoids were obtained and four previously reported β-propanediones were obtained.Through methyl thiazolyl tetrazolium (MTT) The inhibitory effect of 19 compounds on Hela activity of human cervical cancer cells was evaluated in vitro. The results showed that the IC 50 of compound 13 was 19.4 μmol / L, which has the value of further study.