285138-16-1

Upstream product

• 7298-67-1 5-acetamido-2-hydroxyacetophenone 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 103-90-2 4-acetaminophenol 

Downstream Products

• 285138-23-0 N-[3-methoxy-4-oxo-2-(3,4,5-trimethoxy-phenyl)-4H-chromen-6-yl]-acetamide 
• 285138-19-4 N-(3-hydroxy-4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-chromen-6-yl)acetamide 

Relevant academic research and scientific papers

Selected novel 5’-amino-2’-hydroxy-1, 3-diaryl-2- propen-1-ones arrest cell cycle of HCT-116 in G0/G1 phase

A series of 5’-amino-2’-hydroxy-1,3-diaryl-2-propen-1-ones (AC1-AC15) were synthesized by Claisen-Schmidt condensation of 5'-acetamido-2’-hydroxy acetophenone with various substituted aromatic aldehydes. The syn- thesized compounds were characterized by FTIR, 1H NMR and mass spectrometry and evaluated for their selec- tive cytotoxicity using MTT assay on two cancer cell lines namely breast cancer cell line (MCF-7), colon cancer cell line (HCT-116) and one normal kidney epithelial cell line (Vero). Among the tested compounds, AC-10 showed maximum cytotoxic effect on MCF-7 cell line with IC50 value 74.7 ± 3.5 μM. On HCT-116 cells, AC-13 exhibited maximum cytotoxicity with IC50 value 42.1 ± 4.0 μM followed by AC-14 and AC-10 with IC50 values 62 ± 2.3 μM and 95.4 ± 1.7 μM respectively. All tested compounds were found to be safe on Vero cell line with IC50 value more than 200 μM. Based on their highest efficacy on HCT-116, AC-10, AC-13 and AC-14 were selected for mechanistic study on this cell line by evaluating changes nucleomorphological characteristics using acridine orange-ethidium bromide (AOEB) dual stain and by analyzing cell cycle with flow cytometry using propidium iodide stain. In AOEB staining, all three tested compounds showed significant (p 0/G1 phase and by AC-13 in G0/G1 and G2/M phase. The study reflected the potential of AC-10, AC-13 and AC-14 to be the lead molecules for further optimization.

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 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.