Nitrobenzene Compounds Inhibit Expression of VCAM-1

https://doi.org/10.1016/S0960-894X(01)00306-7Get rights and content

Abstract

A series of nitrobenzene compounds has been discovered as potent inhibitors of VCAM-1 expression and, therefore, potential drug candidates for autoimmune and allergic inflammatory diseases. Structure–activity relationship (SAR) studies showed that a nitro group and two other electron-withdrawing groups are essential for these compounds to be potent inhibitors of VCAM-1 expression.

A series of nitrobenzene compounds has been discovered as potent inhibitors of VCAM-1 expression.

  1. Download : Download high-res image (12KB)
  2. Download : Download full-size image

Section snippets

Acknowledgements

The authors thank Dr. J. Sikorski for critically proofreading the manuscript of this publication.

References (24)

  • T.A. Springer

    Cell

    (1994)
  • C.A. Foster

    J. Allergy Clin. Immunol.

    (1996)
  • A.B. Kay

    J. Allergy Clin. Immunol.

    (1991)
  • U. Hommel et al.

    FEBS Lett.

    (1996)
  • R.R. Cobb et al.

    FEBS Lett.

    (1996)
  • S. Kapiotis et al.

    Life Sci.

    (1996)
  • J.W. Pierce et al.

    J. Biol. Chem.

    (1997)
  • E.D. Harris

    N. Engl. J. Med.

    (1990)
  • L. Castano et al.

    Annu. Rev. Immunol.

    (1990)
  • S. Zamvil et al.

    Annu. Rev. Immunol.

    (1990)
  • R. Ross

    N. Engl. J. Med.

    (1986)
  • M.P. Bevilacqua et al.

    Annu. Rev. Med.

    (1994)
  • Cited by (7)

    • Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone

      2011, Journal of Biological Chemistry
      Citation Excerpt :

      It has two electron withdrawing groups (methylsulfonyl and nitro) on the phenyl ring and an ester linkage with the amide group. This MSNB scaffold has only rarely been disclosed in drug discovery (37, 38). In addition, a search of the PubChem BioAssay database showed that MSNB analogs are active against few targets (PubChem AID 1339 for a ras GTPase assay and AIDs 1304, 1359, and 1861 for a neuropeptide Y receptor type 1 assay), despite having been repeatedly screened in the Molecular Libraries Program.

    View all citing articles on Scopus
    View full text