Beta-C-mannosides as selectin inhibitors.

Abstract:

:Potential E- and P-selectin inhibitors were synthesized to explore a hydrophobic area on the E-selectin surface and the PSGL-1 protein binding site on the P-selectin surface that was recently defined by crystallography. Three series of mannose-based compounds (libraries A, B, and C) were synthesized using solution phase parallel synthesis. Biological evaluation of these compounds was done using two ELISA-based assays and transferred NOE (trNOE) experiments. Some of the compounds showed better activity than sLe(x) in the P-selectin assay.

journal_name

J Med Chem

authors

Kaila N,Chen L,Thomas BE 4th,Tsao D,Tam S,Bedard PW,Camphausen RT,Alvarez JC,Ullas G

doi

10.1021/jm010390f

keywords:

subject

Has Abstract

pub_date

2002-04-11 00:00:00

pages

1563-6

issue

8

eissn

0022-2623

issn

1520-4804

pii

jm010390f

journal_volume

45

pub_type

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