402582-10-9Relevant 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.
Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(Aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides
Zhu,Arendsen,Gunawardana,Boyd,Stewart,Fry,Cool,Kifle,Schaefer,Meuth,Marsh,Kempf-Grote,Kilgannon,Gallatin,Okasinski
, p. 3469 - 3487 (2007/10/03)
The elevated expression of cell adhesion molecules (CAMs) on the lumenal surface of vascular endothelial cells is a critical early event in the complex inflammatory process. The adhesive interactions of these CAMs that include E-selectin, ICAM-1, and VCAM
