Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents.
A biological evaluation of the antiadhesive activity of novel heparan sulfate glycosaminoglycans mimetic compounds (KI-compounds) is described. In an adhesion assay, KI-111 [2-(4-fluoro-3-nitrobenzoyl)benzoic acetic anhydride] was found to exert potent inhibitory activities against the adhesion of human fibrosarcoma HT1080 cells and HeLa cells to fibronectin. Cell growth, migration, and invasion of HT1080 cells were also inhibited by KI-111 at almost equal concentrations.
Ishida
Keisuke
K
Antibiotics Laboratory, RIKEN Discovery Research Institute, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
Simizu
Siro
S
Teruya
Takayuki
T
Wierzba
Michal K
MK
Osada
Hiroyuki
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005353:Fibronectins / Q000378:metabolism; D006497:Heparan Sulfate / Q000031:analogs & derivatives* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D018716:Molecular Mimicry; D009361:Neoplasm Invasiveness / Q000517:prevention & control*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D005353:Fibronectins; D006497:Heparan Sulfate