69155-77-7

Upstream product

• 21222-04-8 5'-Acetoxy-2'-hydroxyacetophenone 
• 68-12-2 N,N-dimethyl-formamide 
• 490-78-8 2,5-Dihydroxyacetophenone 

Downstream Products

• 1592003-25-2 5-(2,5-Dihydroxybenzoyl)-1-hexylpyridin-2(1H)-one 
• 1592003-26-3 5-(2,5-dihydroxybenzoyl)-1-isopropylpyridin-2(1H)-one 
• 1592003-27-4 1-hexyl-5-(2-hydroxy-5-methoxybenzoyl)pyridin-2(1H)-one 
• 1592003-28-5 1-cyclohexyl-5-(2-hydroxy-5-methoxybenzoyl)pyridin-2(1H)-one 
• 1592003-29-6 t-butyl [2-{5-(2-hydroxy-5-methoxybenzoyl)-2-oxopyridin-1(2H)-yl}ethyl]carbamate 
• 124980-69-4 β-(6-Acetoxy-3-chromonyl)acrolein 

Relevant academic research and scientific papers

Synthesis, antiproliferative, and c-Src kinase inhibitory activities of 4-oxo-4H-1-benzopyran derivatives

A new class of 4-oxo-4H-1-benzopyran derivatives were synthesized and their antiproliferative activity examined against a panel of three human cancer cell lines, that is, breast carcinoma (MDA-MB-468), ovarian adenocarcinoma (SK-OV-3), and colorectal adenocarcinoma (HT-29). Two compounds, that is, 3-hexyl-7,8-dihydroxy-4-oxo-4H-1-benzopyran and (E)-ethyl 3-(7-methoxy-4-oxo-4H-1-benzopyran-3-yl)acrylate were found to be potent against all three cancer cell lines studied at 50 μM concentration. Also, the inhibitory potency of the compounds was evaluated against active Src kinase. A few of these compounds exhibited modest Src kinase inhibitory activity (IC50 = 52-57 μM). Structure-activity relationship studies with respect to the nature and position of substituents on the lead compounds could be further exploited for the design and development of more potent antiproliferative agents and/or Src kinase inhibitors.

Inhibition of Alzheimer's BACE-1 by 2,6-dialkyl-4-chromon-3-yl-1,4-dihydropyridine-3,5-dicarboxylates

Alzheimer's disease is the most common cause of dementia in the elderly, and no disease-modifying therapy is yet available for this devastating pathology. Deposition of different physicochemical forms of amyloid-β peptides is a critical phase in the patho

Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives

Src kinase, a prototype member of the Src family of kinases (SFKs), is over-expressed in various human tumors, and has become a target for anticancer drug design. In this perspective, a series of eighteen 2-pyridone derivatives were synthesized and evaluated for their c-Src kinase inhibitory activity. Among them, eight compounds exhibited c-Src kinase inhibitory activity with IC 50 value of less than 25 μM. Compound 1-[2-(dimethylamino)ethyl]- 5-(2-hydroxy-4-methoxybenzoyl)pyridin-2(1H)-one (36) exhibited the highest c-Src kinase inhibition with an IC50 value of 12.5 μM. Furthermore, the kinase inhibitory activity of compound 36 was studied against EGFR, MAPK and PDK, however no significant activity was observed at the highest tested concentration (300 μM). These results provide insights for further optimization of this scaffold for designing the next generation of 2-pyridone derivatives as candidate Src kinase inhibitors.