Structure-activity relationships studies of the anti-angiogenic activities of linomide.
The synthesis and anti-angiogenic activities of linomide and its analogues are reported. Three of the analogues are 3.3-69 times more potent than linomide at inhibiting blood vessel formation in the CAM angiogenesis assay. These compounds possessed considerable anti-proliferative activity against isolated HUVEC cells with no activity against epithelial-derived prostate tumor cells.
Shi
Jiandong
J
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Xiao
Zili
Z
Ihnat
Michael A
MA
Kamat
Chandrashekhar
C
Pandit
Bulbul
B
Hu
Zhigen
Z
Li
Pui-Kai
PK
D000481:Allantoin / Q000737:chemistry; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002642:Chick Embryo; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D006801:Humans; D006912:Hydroxyquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D008297:Male; D008566:Membranes / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000187:drug effects; D011471:Prostatic Neoplasms / Q000098:blood supply / Q000473:pathology; D012039:Regional Blood Flow / Q000187:drug effects; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D020533:Angiogenesis Inhibitors; D006912:Hydroxyquinolines; D000481:Allantoin; C045282:roquinimex