Synthesis of prenylated and geranylated xanthones and their bioactivities  

异戊烯基和香叶基取代的呫吨酮的合成与生物活性研究

作　　者：Beidou Zhou Zihan Yu Yugui Tong Jiali Li Baocheng Huang Rongrong Wei Zhimin Weng Xin Wang Zhipeng Ruan Jian Lin Caihong Xu Jianbo Liu 周北斗;俞紫涵;童玉贵;李佳莉;黄堡城;魏蓉蓉;翁智敏;王欣;阮志鹏;林健;许彩红;刘建波(莆田学院药学与医学技术学院,药物分析与检验医学福建省高校重点实验室,福建莆田351100;莆田出入境检验检疫局,福建莆田351100;莆田学院附属医院医疗集团,福建莆田351100;联化科技股份有限公司,浙江台州318020)

机构地区：[1]School of Pharmacy and Medical Technology,Putian University,Key Laboratory of Pharmaceutical Analysis and Laboratory Medicine(Putian University),Fujian Province University,Putian 351100,China [2]Putian Entry-exit Inspection and Quarantine Bureau,Putian 351100,China [3]The Affiliated Hospital(Group)of Putian University,Putian 351100,China [4]Lianhe Chemical Technology Co.,Ltd.,Taizhou 318020,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2020年第8期564-576,共13页中国药学（英文版）

基　　金：Leading Project of Fujian Provincial Department of Science and Technology(Grant No.2018Y0072)。

摘　　要：Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated.Compound 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin.Compounds 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described above.These results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.通过两步反应,合成了9个异戊烯基和香叶基取代的呫吨酮类化合物,总产率在11%到36%之间。所有的化合物均为首次报道。然后对化合物1–9的全部或者部分抗肿瘤、抑制酪氨酸酶、抑制胰脂肪酶、抗真菌和抗菌活性进行评估。化合物9显示出明显的抗肿瘤活性,其对人乳腺癌细胞MCF-7和MDA-MB-231的细胞毒性均大于顺铂。化合物1–4和6–7也显示出一定的上述除了抗肿瘤以外的活性。这些结果显示化合物1–4、6–7和9是很有希望的先导化合物,可用于进一步结构修饰。

关 键 词：XANTHONE Antitumor activity Anti-tyrosinase Antifungal activity Antibacterial activity 

分 类 号：R915.4[医药卫生—微生物与生化药学]