Synthesis and antithrombotic activity of carbolinecarboxyl RGD sequence.
3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid, RGDS, RGDV, RGDF and their linkers were synthesized. The anti-aggregation and adhesion of platelet indicated that the in vitro activities of the linkers remained at the same level as RGDS, RGDV, and RGDF (p>0.05). The antithrombotic activities in vivo suggested, however, that the potencies of RGDS, RGDV and RGDF were enhanced by the introduction of 3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxyl group into their alpha amino group (p<0.05, 0.01 or 0.001).
Lin
Na
N
College of Pharmaceutical Sciences, Peking University, 100083, Beijing, PR China.
Zhao
Ming
M
Wang
Chao
C
Peng
Shiqi
S
D000818:Animals; D002243:Carbolines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects; D004195:Disease Models, Animal; D005343:Fibrinolytic Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008297:Male; D009842:Oligopeptides / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000188:drug therapy; D014407:Tumor Cells, Cultured / Q000187:drug effects
D002243:Carbolines; D005343:Fibrinolytic Agents; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid