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设计、合成及鉴定新型三芳基甲胺类化合物作为载脂蛋白 E 生成抑制剂。

Design, synthesis and identification of a new class of triarylmethyl amine compounds as inhibitors of apolipoprotein E production.

机构信息

Department of Chemistry, California State University Fresno, Fresno, CA 93740, USA.

出版信息

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6252-5. doi: 10.1016/j.bmcl.2012.08.009. Epub 2012 Aug 10.

Abstract

We have identified a new class of triarylmethyl amine compounds that can inhibit apolipoprotein E (apoE) production. ApoE is a cholesterol- and lipid-carrier protein implicated in aging, atherosclerosis, Alzheimer's Disease (AD), and other neurological and lipid-related disorders. Attenuation of apoE production is generally considered to be of therapeutic value. A majority of the apoE in the brain is produced by astrocytes. Here, we describe the design, synthesis, and biological screening of a small library of compounds that led to the identification of four triarylmethyl amines as potent inhibitors of apoE production in CCF-STTG1 astrocytoma cells.

摘要

我们已经确定了一类新的三芳基甲胺化合物,它们可以抑制载脂蛋白 E(apoE)的产生。apoE 是一种胆固醇和脂质载体蛋白,与衰老、动脉粥样硬化、阿尔茨海默病(AD)和其他神经和脂质相关疾病有关。降低 apoE 的产生通常被认为具有治疗价值。大脑中的大多数 apoE 是由星形胶质细胞产生的。在这里,我们描述了一个化合物文库的设计、合成和生物学筛选,这些化合物导致了四种三芳基甲胺作为 CCF-STTG1 星形胶质细胞瘤细胞中 apoE 产生的有效抑制剂的鉴定。

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