Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates

…, Y Nagano, A Matsuura, A Kohara, S Ninomiya…

Index: Suzuki, Takayoshi; Nagano, Yuki; Matsuura, Azusa; Kohara, Arihiro; Ninomiya, Shin-Ichi; Kohda, Kohfuku; Miyata, Naoki Bioorganic and Medicinal Chemistry Letters, 2003 ,  vol. 13,  # 24  p. 4321 - 4326

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Citation Number: 47

Abstract

In order to find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, a series of compounds modeled after suberoylanilide hydroxamic acid (SAHA) were designed and synthesized as (i) substrate (acetyl lysine) analogues (compounds 3–7),(ii) analogues bearing various functional groups expected to chelate zinc ion (compounds 8–15), and (iii) analogues bearing nucleophilic functional groups which could bind covalently to HDACs ( ...