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Synthesis of a Cosalane Analog With an Extended Polyanionic Pharmacophore Conferring Enhanced Potency As an Anti-Hiv Agent

  1. Author:
    Cushman, M.
    Insaf, S.
    Ruell, J. A.
    Schaeffer, C. A.
    Rice, W. G.
    1. Year: 1998
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 8
    2. 7
    3. Pages: 833-836
  4. Type of Article: Article
  1. Abstract:

    A novel cosalane analog having an extended polyanionic pharmacophore was synthesized in order to target specific cationic residues on the surface of CD4. The design rationale is based on a hypothetical binding model of cosalane to the surface of the protein. The new analog displayed an EC50 of 0.55 mu M as an inhibitor of the cytopathic effect of HIV-1(RF) in CEM-SS cells, which represents a significant increase in potency over cosalane itself (EC50 5.1 mu M) Both cosalane and the new analog are inhibitors of viral entry into target cells. (C) 1998 Elsevier Science Ltd. All rights reserved. [References: 15]

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