摘要:
在当前的研究中,5个氟取代和3个氯取代的1,3-二羟基氧杂蒽酮(化合物11-18)被一步合成,它们的产率在48%和72%之间.在这8个化合物中,化合物12和15-18被首次报道.化合物1-19的全部或者部分抗肿瘤、抑制酪氨酸酶和抑制血小板聚集的活性被检测.对于某些特定的肿瘤细胞,化合物1-2、4、6-7、10-15和19显示出较好的抑制活性,特别是7位含有2,4-二氟苯基的化合物10显示出较高的抗肿瘤活性.化合物18对酪氨酸酶的抑制率约为22%.在大鼠中,化合物1-3、6、9、12和18-19明显地抑制由二磷酸腺苷(ADP)诱导的血小板聚集.而且,化合物2和3的作用最为显著.这些结果显示化合物1-4、6-7、9-15和19是有希望的先导化合物,可用于进一步结构修饰.%In the present study,five fluorine substituted and three chlorine substituted 1,3-dihydroxyxanthones were synthesized in one step.The yields ranged from 48% to 72%.Among them,compounds 12 and 15-18 were reported for the first time.The antitumor,antityrosinase and antiplatelet aggregation activities of all or part of compounds 1-19 were evaluated.Compounds 1,2,4,6-7,10-15 and 19 exhibited enhanced cytotoxicity against certain cancer cells.Compound 10,containing 2,4-difluorophenyl at the C7 position,particularly exhibited superior antitumor activity.The inhibition rate of compound 18 against tyrosinase was approximately 22%.Compounds 1-3,6,9,12 and 18,19 exhibited obvious inhibitory platelet aggregation induced by ADP in rats.Moreover,the effects of compounds 2 and 3 were more pronounced.These results demonstrated that compounds 1-4,6-7,9-15 and 19 were promising leads for further structural modification.