title: Design, synthesis and identification of a new class of triarylmethyl amine compounds as inhibitors of apolipoprotein E production.
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.
authors.affiliation: Department of Chemistry, California State University Fresno, Fresno, CA 93740, USA.
authors.forename: Mandeep
authors.initials: M
authors.lastname: Singh
authors.forename: Jason T
authors.initials: JT
authors.lastname: Schott
authors.forename: Martin A
authors.initials: MA
authors.lastname: Leon
authors.forename: Robert T
authors.initials: RT
authors.lastname: Granata
authors.forename: Harkiran K
authors.initials: HK
authors.lastname: Dhah
authors.forename: Jason A
authors.initials: JA
authors.lastname: Welles
authors.forename: Michelle A
authors.initials: MA
authors.lastname: Boyce
authors.forename: Hafeez S
authors.initials: HS
authors.lastname: Oseni-Olalemi
authors.forename: Charles E
authors.initials: CE
authors.lastname: Mordaunt
authors.forename: Anthony J
authors.initials: AJ
authors.lastname: Vargas
authors.forename: Nilay V
authors.initials: NV
authors.lastname: Patel
authors.forename: Santanu
authors.initials: S
authors.lastname: Maitra
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001057:Apolipoproteins E / Q000096:biosynthesis*; D001254:Astrocytoma / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000588:Amines; D001057:Apolipoproteins E; D054852:Small Molecule Libraries