Synthesis and evaluation of graveoline and graveolinine derivatives with potent anti-angiogenesis activities.
A series of graveoline and graveolinine derivatives were synthesized. The biological results showed that most of graveoline derivatives possessed higher cytotoxicity and better inhibitive effect against the adhesion and migration of human umbilical vein endothelial cell (HUVEC) than graveolinine derivatives. Among these compounds, 8d was the most potent agents that also showed significant anti-angiogenesis activities in chick embryo chorioallantoic membrane (CAM) assay.
An
Zeng-Yun
ZY
School of Pharmaceutical Sciences, Sun Yat-sen University, Waihuan East Road 132, Guangzhou 510080, China.
Yan
Yi-Yong
YY
Peng
Dan
D
Ou
Tian-Miao
TM
Tan
Jia-Heng
JH
Huang
Shi-Liang
SL
An
Lin-Kun
LK
Gu
Lian-Quan
LQ
Huang
Zhi-Shu
ZS
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D002642:Chick Embryo; D049033:Chorioallantoic Membrane / Q000187:drug effects; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects; D006801:Humans; D008730:Methoxsalen / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
D020533:Angiogenesis Inhibitors; D015363:Quinolones; C487585:graveoline; D008730:Methoxsalen