Method of inhibiting apolipoprotein-e expression comprising administering a triarylmethyl amine compound
a technology of triarylmethyl amine and apolipoprotein, which is applied in the direction of biocide, tumor/cancer cells, artificial cell constructs, etc., can solve the problems that alzheimer's disease will continue to be a major and expensive health crisis
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example 1
Synthesis of Triarylmethyl amine 4-(Naphthalen-2-yl-diphenyl-methyl)-morpholine (Shown as Compound 33 in Table 1)
[0043]Scratched magnesium turnings (1.056 g, 43.4 mmol) were placed in a 250 mL round-bottomed, 3-neck flask at room temperature. A small portion of the solution of 2-bromonaphthalene (11.84 g, 47.7 mmol) in anhydrous ether (40 mL) was added through an addition funnel and the solution was heated to gentle reflux maintaining the temperature at 35° C. The rest of the solution was added in small fractions over a period of 1 hour, and the resulting reaction mixture was refluxed for an additional 1 hour. Disappearance of all magnesium indicated the completion of the reaction.
[0044]The solution containing benzophenone (7.04 g, 38.6 mmol) in anhydrous ether (20 mL) was added through an additional funnel all at once over 2-4 minutes. The resulting reaction was gently refluxed for 24 hours. The cooled mixture was slowly and carefully quenched by adding aqueous HCl (6M) to the rea...
example 2
Synthesis of Triarylmethyl amine: Diethyl-[(4-methoxy-phenyl)-diphenyl-methyl]-amine (Shown as Compound 17 in Table 1)
[0047]The reaction was carried out on a 1 / 10th scale compared to EXAMPLE 1, starting with scratched magnesium turnings (0.110 g, 4.3 mmol) placed in a 250 mL round-bottomed, 3-neck flask at room temperature. A small portion of the solution of 2-bromonaphthalene (1.18 g, 47.7 mmol) in anhydrous ether (4 mL) was added through an addition funnel and the solution was heated to gentle reflux maintaining the temperature at 35° C. The rest of the solution was added in small fractions over a period of 1 hour, and the resulting reaction mixture was refluxed for an additional 1 hour. Disappearance of all magnesium indicated the completion of the reaction.
[0048]The solution containing benzophenone (0.7 g, 38.6 mmol) in anhydrous ether (2 mL) was added through an additional funnel over 2-4 minutes. The resulting reaction was gently refluxed for 24 hours. The cooled mixture was ...
example no.3
EXAMPLE NO. 3
Triarylmethyl Amine Compounds Administered to Human CCF-STTG1 Astrocytoma Cells and Analyzed by ELISA
[0060]To obtain the data shown in Table 2, Table 3, and FIG. 2, the human CCF-STTG1 astrocytoma cells (ATCC, CRL-1718) were maintained in RPMI medium (Mediatech) supplemented with 10 mM HEPES, 1 mM sodium pyruvate, 4.5 g / L glucose, 1% penicillin / streptomycin, and 10% bovine growth serum (HyClone) at 37° C. with 5% CO2.
[0061]All triarylmethyl amine compounds listed in Table 1 were individually dissolved in DMSO at a stock concentration of 10 mM and individually tested. For ELISA's, 1.6×104 cells / 96-well were grown for 1 day in RPMI, followed by a 24 hour equilibration in serum-free Opti-MEM (Life Technologies). Treatments were carried out in quadruplicate with 100 μL of fresh Opti-MEM containing 10 μM of compound or vehicle (0.1% DMSO) for 24 hours. Conditioned medium from these samples were then diluted 2-fold with incubation buffer (PBS+0.05% Tween-20+0.1% BSA) and anal...
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