285138-18-3

Upstream product

• 95428-17-4 5′-acetamino-3-(3,4-dimethoxyphenyl)-2′-hydroxychalcone 
• 103-90-2 4-acetaminophenol 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 7298-67-1 5-acetamido-2-hydroxyacetophenone 
• 95428-17-4 acetic acid-[3-(3,4-dimethoxy-trans-cinnamoyl)-4-hydroxy-anilide] 

Downstream Products

• 285138-22-9 N-(2-(3,4-dimethoxyphenyl)-3-methoxy-4-oxo-4H-chromen-6-yl)acetamide 

Relevant academic research and scientific papers

COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES

This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

Synthesis and anti-cancer activity of novel thiazolidinone analogs of 6-aminoflavone

Novel heterocyclic analogs were synthesized by combining a flavone nucleus and thiazolidinone ring in an effort to potentiate the existing anti-cancer activity of flavone. The syntheses of 6-aminoflavone, 6-amino-3-methoxyflavone, 6-amino-3-methoxy-3',4'-dimethxyflavone and their corresponding thiazolidinone analogs were performed. Fifteen novel analogs were synthesized and evaluated for their anti-cancer activity using cell-based assay techniques and in vivo testing. As expected, the analogs improved cytotoxicity and were shown to increase the life span of cancer-bearing mice. Cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assays in HeLa, MDA-MB-435, and Vero cell lines. In vivo evaluation of anti-cancer activity performed in albino mice bearing Dalton's ascites carcinoma showed that the new analogs enhanced life span and prevented increases in body weight owing to tumor volumes. Moreover, cell-cycle analysis and Hoechst staining analysis proved the apoptotic potential of these analogs. Preliminary pharmacokinetic evaluation was carried out on the synthesized compounds to determine the lipophilicity and pKa. Lipophilicity was determined using high-performance liquid chromatography and the results showed a direct correlation between the observed anti-cancer activity and log P value, while pKa values indicated the ionizing range which is a prediction tool for solubility and permeability.

Synthesis of some new 6-amino-3-methoxyflavones

Several naturally occurring flavones having 3-methoxy group are known for their biological activities. Here we report the synthesis of some new flavones starting from 5-acetamido-2-hydroxyacetophenone.