当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.

Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.

Abstract：

: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 circulating leukocytes to the site of the inflammation. These adhesive interactions allow the leukocytes to firmly adhere to and cross the vascular endothelium and migrate to the site of tissue injury. Pharmaceutical agents which would prevent the induced expression of one or more of the cell adhesion molecules on the endothelium might be expected to provide a novel mechanism to attenuate the inflammatory responses associated with chronic inflammatory diseases. A thieno[2,3-d]pyrimidine, A-155918, was identified from a whole-cell high-throughput assay for compounds which inhibited the tumor necrosis factor-alpha (TNFalpha)-induced expression of E-selectin, ICAM-1, or VCAM-1 on human vascular endothelial cells. Traditional medicinal chemistry methods were applied to this low-micromolar inhibitor, resulting in the 2,4-disubstituted thieno[2,3-c]pyridine A-205804, a potent and selective lead inhibitor of E-selectin and ICAM-1 expression (IC(50) = 20 and 25 nM, respectively). The relative position of the nitrogen atom in the thienopyridine isomer was shown to be critical for activity, as was a small amide 2-substituent.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Stewart AO,Bhatia PA,McCarty CM,Patel MV,Staeger MA,Arendsen DL,Gunawardana IW,Melcher LM,Zhu GD,Boyd SA,Fry DG,Cool BL,Kifle L,Lartey K,Marsh KC,Kempf-Grote AJ,Kilgannon P,Wisdom W,Meyer J,Gallatin WM,Okasinski G

doi

10.1021/jm000452m

keywords:

subject

Has Abstract

pub_date

2001-03-15 00:00:00

pages

988-1002

issue

6

eissn

0022-2623

issn

1520-4804

pii

jm000452m

journal_volume

44

pub_type

杂志文章

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