52923-34-9

Upstream product

• 103-90-2 4-acetaminophenol 
• 51-66-1 4-methoxyacetanilide 
• 104-94-9 4-methoxy-aniline 
• 7298-67-1 5-acetamido-2-hydroxyacetophenone 
• 100-52-7 benzaldehyde 

Downstream Products

• 109093-42-7 N-(3-hydroxy-4-oxo-2-phenyl-4H-chromen-6-yl)acetamide 
• 18467-10-2 N-(4-oxo-2-phenyl-4H-chromen-6-yl)acetamide 
• 4613-53-0 6-amino-2-phenyl-4H-1-benzopyran-4-one 
• 1245282-84-1 N-(3-methoxy-4-oxo-2-phenyl-4H-chromen-6-yl)acetamide 

Relevant academic research and scientific papers

AHR INHIBITORS AND USES THEREOF

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

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.

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.

Anti-HIV and antiplasmodial activity of original flavonoid derivatives

In our search for potent anti-HIV and antiplasmodial agents, novel series of flavonoid derivatives and their chalcone intermediates were synthesized and evaluated for inhibition of HIV multiplication and antiproliferative activity on Plasmodium falciparum