Lead discovery of α,β-Unsaturated sulfones from a combinatorial library as inhibitors of inducible VCAM-1 expression

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Abstract

α,β-Unsaturated sulfones have been discovered from a combinatorial library as leads for a new series of inhibitors of inducible VCAM-1 expression. Although not essential, further conjugation of the sulfonyl group to another vinyl group or a phenyl group increases the potency dramatically.

α,β-Unsaturated sulfones have been discovered from a combinatorial library as leads for a new series of inhibitors of inducible VCAM-1 expression.

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Acknowledgements

We would like to thank Drs. J. Sikorski and W. D. Weingarten for fruitful discussions and critical proofreading of the manuscript of this publication.

References (13)

  • T.A. Springer

    Cell

    (1994)
  • C.A. Foster

    J. Allergy Clin. Immunol.

    (1996)
  • E.D. Harris

    N. Engl. J. Med.

    (1990)
  • L. Castano et al.

    Annu. Rev. Immunol.

    (1990)
  • S. Zamvil et al.

    Annu. Rev. Immunol.

    (1990)
  • M.P. Bevilacqua et al.

    Annu. Rev. Med.

    (1994)
There are more references available in the full text version of this article.

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