CAS: 218457-76-2; Fmoc-Asu-Oh

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4254-88-0 250384-77-1 218457-78-4

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CAS号4254-88-0 (S)-2-氨基辛二酸 | CAS号82911-69-1 9-芴甲基-N-琥珀酰亚胺碳酸酯

📜(S)-2-氨基辛二酸,9-芴甲基-N-琥珀酰亚胺基碳酸酯置于碳酸氢钠体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 20.0H,以100%的收率获得fmoc-L-2-氨基辛二酸
参考文献:Solid Phase Synthesis Of Hydroxamate Peptides For Histone Deacetylase Inhibition
标题:Solid Phase Synthesis Of Hydroxamate Peptides For Histone Deacetylase Inhibition
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),Currently Being Used To Treat A Variety Of Human Cancers. This Strategy Was Employed To Synthesize A Series Of Nonameric Peptides Related To Actual Hdac Substrates,Derived From Known Sites Of Acetylation/deacetylation On The N-Terminal Tails Of The Histone Core Proteins H2A,H2B,H3,And H4. In Each Case The Lysine Residue Was Replaced By A Hydroxamate-Bearing Side Chain,To Mimic The Endogenous Site Of Deacetylation. Mass Spectrometry And High Performance Liquid Chromatography (HPLC) Confirmed The Success Of Automated Solid-Phase Synthesis. These Results Suggest Facile Synthesis Of A New Class Of Hdac Inhibitors That May Have Enhanced Selectivity For Specific Hdac Isoforms. (C) 2012 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tetlet.2012.10.113