Thiazole-and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase

…, M Pallavicini, SK Bernini, G Chiodini, A Corsini…

文献索引：Bolchi, Cristiano; Pallavicini, Marco; Bernini, Sergio K.; Chiodini, Giuseppe; Corsini, Alberto; Ferri, Nicola; Fumagalli, Laura; Straniero, Valentina; Valoti, Ermanno Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5408 - 5412

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被引用次数: 13

摘要

Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4- thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl-and 2-methylmercapto-4- thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4- thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed ...