Design, synthesis, and pharmacological evaluation of new farnesyl protein transferase inhibitors

…, JF Goossens, P Chavatte, JP Hénichart

文献索引：Houssin, Raymond; Pommery, Jean; Salauen, Marie-Catherine; Deweer, Sophie; Goossens, Jean-Francois; Chavatte, Philippe; Henichart, Jean-Pierre Journal of Medicinal Chemistry, 2002 , vol. 45, # 2 p. 533 - 536

全文：HTML全文

被引用次数: 27

摘要

New CA1A2X 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 ...