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Bioorg Med Chem Lett ; 22(19): 6252-5, 2012 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-22959206

RESUMEN

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.


Asunto(s)
Aminas/farmacología , Apolipoproteínas E/biosíntesis , Diseño de Fármacos , Bibliotecas de Moléculas Pequeñas/síntesis química , Bibliotecas de Moléculas Pequeñas/farmacología , Aminas/síntesis química , Aminas/química , Astrocitoma/metabolismo , Astrocitoma/patología , Línea Celular Tumoral , Humanos , Estructura Molecular , Bibliotecas de Moléculas Pequeñas/química
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