A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti- proliferative and anti-inflammatory activities

Tapadar Subhasish; Fathi Shaghayegh; Raji IdrisOmesiete WilsonKornacki James R.Mwakwari Sandra C.Miyata MasanoriMitsutake KazunoriLi Jian-DongMrksich MilanOyelere Adegboyega K.

首页> 外文期刊>Bioorganic and medicinal chemistry >A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti- proliferative and anti-inflammatory activities

【24h】

A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti- proliferative and anti-inflammatory activities

机译：A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti- proliferative and anti-inflammatory activities

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相关主题

摘要

Inhibition of the enzymatic activity of histone deacetylase (HDAC) is a promising therapeutic strategy for cancer treatment and several distinct small molecule histone deacetylase inhibitors (HDACi) have been reported. We have previously identified a new class of non-peptide macrocyclic HDACi derived from 14- and 15-membered macrolide skeletons. In these HDACi, the macrocyclic ring is linked to the zinc chelating hydroxamate moiety through a para-substituted aryl-triazole cap group. To further delineate the depth of the SAR of this class of HDACi, we have synthesized series of analogous compounds and investigated the influence of various substitution patterns on their HDAC inhibitory, anti-proliferative and anti-inflammatory activities. We identified compounds 25b and 38f with robust anti-proliferative activities and compound 26f (IC50 47.2 nM) with superior anti-inflammatory (IC50 88 nM) activity relative to SAHA. (C) 2015 Elsevier Ltd. All rights reserved.

著录项

来源
《Bioorganic and medicinal chemistry》 |2015年第24期|7543-7564|共22页
作者
Tapadar Subhasish; Fathi Shaghayegh; Raji IdrisOmesiete WilsonKornacki James R.Mwakwari Sandra C.Miyata MasanoriMitsutake KazunoriLi Jian-DongMrksich MilanOyelere Adegboyega K.;
展开▼
作者单位

Georgia Inst Technol, Sch Chem & Biochem, Parker H Petit Inst Bioengn & Biosci, Atlanta, GA 30332;

Northwestern Univ, Dept Chem, Evanston, IL 60208 USA;

Georgia State Univ, Ctr Inflammat Immun & Infect, Inst Biomed Sci, Atlanta, GA 30303 USA;

展开▼
收录信息
原文格式 PDF
正文语种英语
中图分类药学;
关键词
Histone deacetylase (HDAC); Histone deacetylase inhibitors (HDACi); Non-peptide macrocyclic HDACi; Anti-cancer; Structure activity relationship study (SAR); Anti-inflammation; NTHi; NF-kappa B;

A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti- proliferative and anti-inflammatory activities

摘要

著录项

相关主题

期刊订阅