文章基本信息

标题：Synthesis and Biological Evaluation of FTY720 (Fingolimod) Derivatives with Aromatic Head Group as Anticancer Agents
作者：Taeho Lee ; Hong Seop Moon ; Seon Woong Kim 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2018
卷号：66
期号：10
页码：1015-1018
DOI：10.1248/cpb.c18-00065
语种：English
出版社：The Pharmaceutical Society of Japan
摘要：FTY720 is employed for the treatment of multiple sclerosis and exerts apoptotic effects on various cancers through protein phosphatase 2A (PP2A) activation. In compound 4 , the dihydroxy head group of FTY720 was modified into dihydroxy phenyl group. The cell survival in compound 4 treated colorectal and gastric cancer cells was significantly reduced as compared with control, 34.6 and 25.1%, respectively. The docking study of compound 4 showed that the aromatic head group effectively binds to PP2A.
关键词：FTY720;fingolimod;anticancer;sphingosine kinase;derivative