文献类型：期刊文章

作　　者：周北斗[1] 王欣[1] 翁智敏[1] 黄堡城[1] 马泽通[1] 于博[1] 阮丽琴[1] 胡栋宝[2]

机构地区：[1]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 [2]玉溪师范学院化学生物与环境学院,云南玉溪653100

出　　处：《Journal of Chinese Pharmaceutical Sciences》

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

年　　份：2019

卷　　号：28

期　　号：4

起止页码：247-256

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2019_2020、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：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.

关 键 词：XANTHONE SYNTHESIS ANTITUMOR Antityrosinase  ANTIPLATELET AGGREGATION

分 类 号：R916[药学类]