Tetrahedron Letters

Solid phase synthesis of hydroxamate peptides for histone deacetylase inhibition

DM Wilson, LN Silverman, M Bergauer, KR Keshari

文献索引：Wilson, David M.; Silverman, Lisa N.; Bergauer, Markus; Keshari, Kayvan R. Tetrahedron Letters, 2013 , vol. 54, # 2 p. 151 - 153

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被引用次数: 5

摘要

An orthogonal protecting group strategy was devised to synthesize hydroxamic acid containing peptides for biomimetic histone deacetylase (HDAC) inhibition. The basic building block was a protected aminosuberic acid (Asu) derivative bearing a protected hydroxamate in the side-chain, related closely to HDAC inhibitors that are transition-state analogs of acetyllysine. These inhibitors include suberoylanilide hydroxamic acid (SAHA), ...