402582-08-5Relevant academic research and scientific papers
Synthesis and mode of action of 125I- and 3H-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression
Zhu, Gui-Dong,Schaefer, Verlyn,Boyd, Steven A.,Okasinski, Gregory F.
, p. 943 - 948 (2007/10/03)
A series of thieno[2,3-c]pyridine antagonists of cell adhesion molecule (CAM) expression, such as A-205804 (1) and A-249377 (2), selectively suppressed the induced expression of E-selectin and ICAM-1 over VCAM-1. In an effort to explore the biological mechanism of action of these inhibitors, we synthesized 125I- and 3H-labeled thieno[2,3-c]pyridines 5 and 6. An isolated diazonium tetrafluoroborate salt efficiently trapped Na125I on very small scale (7.5 μg of Na125I), providing the corresponding 125I-labeled thieno[2,3-c]pyridine in modest yield. Preliminary mechanistic investigations using these radiolabeled compounds revealed that, upon incubation with human umbilical vein endothelial cells (HUVECs), these inhibitors of CAM expression translocated to the cell nucleus and were noncovalently associated with macromolecules of molecular weight greater than 650 kDa.
Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression
Stewart,Bhatia,McCarty,Patel,Staeger,Arendsen,Gunawardana,Melcher,Zhu,Boyd,Fry,Cool,Kiflie,Lartey,Marsh,Kempf-Grote,Kilgannon,Wisdom,Meyer,Gallatin,Okasinskit
, p. 988 - 1002 (2007/10/03)
A critical early event in the inflammatory cascade is the induced expression of cell adhesion molecules on the lumenal surface of vascular endothelial cells. These adhesion molecules include E-selectin, ICAM-1, and VCAM-1, which serve to recruit circulati
