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

作者信息

Suzuki Takayoshi, Nagano Yuki, Matsuura Azusa, Kohara Arihiro, Ninomiya Shin-ichi, Kohda Kohfuku, Miyata Naoki

机构信息

Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.

出版信息

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4321-6. doi: 10.1016/j.bmcl.2003.09.048.

DOI:10.1016/j.bmcl.2003.09.048
PMID:14643318
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 (compounds 16-18). In this series, semicarbazide 8b and bromoacetamides 18b,c were found to be potent HDAC inhibitors for non-hydroxamates.

摘要

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