Design, synthesis, and pharmacological evaluation of new farnesyl protein transferase inhibitors. |
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| Authors: | Raymond Houssin Jean Pommery Marie-Catherine Salaün Sophie Deweer Jean-Fran?ois Goossens Philippe Chavatte Jean-Pierre Hénichart |
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| Affiliation: | Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille, France. |
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| Abstract: | New CA(1)A(2)X peptidomimetics are described as Ras farnesyl transferase inhibitors (FTIs). They include cysteine and methionine as mimetics of the C-terminus sequence of farnesylated proteins. Furthermore, cysteine was replaced by heterocycles, taking into account the role of zinc and the metabolic instability of amino acids. The molecular docking of 8 in the active site of the enzyme and the pharmacological evaluation of the compounds are illustrative of a new class of FTIs. |
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