氧杂蒽酮的合成和抗肿瘤、抑制酪氨酸酶和抑制血小板聚集活性研究（英文）

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。

Synthesis and antitumor,antityrosinase, and antiplatelet aggregation activities of xanthone

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.