Tetrahedron

Development of a tripeptide mimetic strategy for the inhibition of protein farnesyltransferase

…, J Ohkanda, JW Lockman, Y Qian, MA Blaskovich…

文献索引：Kothare, Mohit A.; Ohkanda, Junko; Lockman, Jeffrey W.; Qian, Yimin; Blaskovich, Michelle A.; Sebti, Said M.; Hamilton, Andrew D. Tetrahedron, 2000 , vol. 56, # 50 p. 9833 - 9841

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被引用次数: 21

摘要

This paper describes the development of a novel terphenyl-based tripeptide mimetic of the CAAX carboxy terminal sequence of Ras. We employ a concise synthesis to form a series of differently functionalized terphenyl inhibitors of protein farnesyltransferase (PFTase), exemplified by 5, 6 and 7. The key reaction in the synthesis of the terphenyl methyl ester 13, and therefore 6 and 7, was the Pd-catalyzed chemoselective Suzuki cross-coupling of 3- ...