Author/Authors :
Christopher J. Dinsmore*، نويسنده , , Theresa M. Williams، نويسنده , , Kelly Hamilton، نويسنده , , Timothy J. OʹNeill، نويسنده , , Elaine Rands، نويسنده , , Kenneth S. Koblan، نويسنده , , Nancy E. Kohl، نويسنده , , Jackson B. Gibbs، نويسنده , , Samuel L. Graham، نويسنده , , George D. Hartman، نويسنده , , Allen I. Oliff، نويسنده ,
Abstract :
The design and synthesis of simple nonpeptide inhibitors of farnesyl-protein transferase (FTase) are described. Cysteine-derived diarylether frameworks are appropriate structural replacements for the C-terminal tetrapeptide portion of the Ras protein, and possess in vitro potency against FTase. Inhibitory activity is dependent on the ring-substitution pattern, and does not require the presence of a C-terminal carboxylate group. © 1997 Elsevier Science Ltd.
