TY - JOUR
T1 - Novel synthetic RGD analogs incorporating salicylic acid derivatives show antiplatelet activity in vitro
AU - Sarigiannis, Yiannis M.
AU - Stavropoulos, George P.
AU - Liakopoulou-Kyriakides, Maria T.
AU - Makris, Pantelis E.
PY - 2002
Y1 - 2002
N2 - Continuing our investigational efforts for more active GpIIb/IIIa inhibitors we have synthesized four novel RGD (Arg-Gly-Asp) analogs incorporating salicylic acid derivatives at their N-terminal amino group using the solid phase synthesis. The synthesized compounds 5-Cl-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 and 5-Br-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 were tested for their inhibitory activity on human platelet aggregation in vitro and found to be potent inhibitors of the platelet aggregation with 75 and 67% inhibitory activity respectively. In order to confirm our results flow cytometry with monoclonal antibodies against GpIb, GpIIb/IIIa, GpIIIa and GMP140 receptors was used.
AB - Continuing our investigational efforts for more active GpIIb/IIIa inhibitors we have synthesized four novel RGD (Arg-Gly-Asp) analogs incorporating salicylic acid derivatives at their N-terminal amino group using the solid phase synthesis. The synthesized compounds 5-Cl-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 and 5-Br-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 were tested for their inhibitory activity on human platelet aggregation in vitro and found to be potent inhibitors of the platelet aggregation with 75 and 67% inhibitory activity respectively. In order to confirm our results flow cytometry with monoclonal antibodies against GpIb, GpIIb/IIIa, GpIIIa and GMP140 receptors was used.
KW - GpIIb/IIIa inhibitors
KW - Inhibitory activity
KW - Platelet aggregation
KW - RGD analogs
KW - Salicylic acid derivatives
UR - http://www.scopus.com/inward/record.url?scp=0242500413&partnerID=8YFLogxK
U2 - 10.1023/A:1024101218318
DO - 10.1023/A:1024101218318
M3 - Article
AN - SCOPUS:0242500413
SN - 0929-5666
VL - 9
SP - 101
EP - 109
JO - Letters in Peptide Science
JF - Letters in Peptide Science
IS - 2-3
ER -