952202-83-4

Upstream product

• 345948-98-3 3-bromo-4-tosyloxy-coumarin 
• 5720-07-0 4-methoxyphenylboronic acid 
• 104-01-8 4-Methoxyphenylacetic acid 
• 119-36-8 methyl salicylate 
• 1276694-79-1 p-methoxyphenylacetic acid 2-(methoxycarbonyl)phenyl ester 
• 26151-95-1 4-hydroxy-3-(4-methoxyphenyl)-2H-chromen-2-one 
• 98-59-9 p-toluenesulfonyl chloride 
• 1076-38-6 4-hydroxy[1]benzopyran-2-one 
• 2650-14-8 3-bromo-4-hydroxycoumarin 

Downstream Products

• 118545-71-4 3-(4-methoxyphenyl)-4-phenyl-2H-chromen-2-one 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 3-substituted 4-anilino-coumarin derivatives as antitumor agents

Various 3-substituted 4-anilino-coumarin derivatives have been designed, synthesized and their anti-proliferative properties have been studied. The in vitro cytotoxicity screening was performed against MCF-7, HepG2, HCT116 and Panc-1 cancer cell lines by MTT assay. Most of the synthesized compounds exhibited comparable anti-proliferative activity to the positive control 5-Fluorouracil against these four tested cancer cell lines. Among the different substituents at C-3 position of coumarin scaffold, 3-trifluoroacetyl group showed the most promising results. Especially, compounds 33d (IC50?=?16.57, 5.45, 4.42 and 5.16?μM) and 33e (IC50?=?20.14, 6.71, 4.62 and 5.62?μM) showed excellent anti-proliferative activities on MCF-7, HepG2, HCT116 and Panc-1 cell lines respectively. In addition, cell cycle analysis and apoptosis activation revealed that 33d induced G2/M phase arrest and apoptosis in MCF-7 cells in a dose-dependent manner. Low toxicity of compounds 33d and 33e was observed against human umbilical vein endothelial cells (HUVECs), suggesting their acceptable safety profiles in normal cells. Furthermore, the results of in silico ADME studies indicated that both 33d and 33e exhibited good pharmacokinetic properties.

3-aryl-4-arylamine-coumarin derivative and preparing method and medical application thereof

The invention relates to the field of medicinal chemistry, in particular to a series of 3-aryl-4-arylamine-coumarin derivatives and a preparing method and medical application thereof, especially medicine applied to curing cancer like breast cancer. A structural formula of a 3-aryl-4-arylamine-coumarin derivative compound is as follow, and definitions of all radical groups in the formula are shown in instructions in details. The structural formula is shown in the specification.

General and efficient route for the synthesis of 3,4-disubstituted coumarins via Pd-catalyzed site-selective cross-coupling reactions

(Chemical Equation Presented) Palladium-catalyzed site-selective cross-coupling reactions of 3-bromo-4-trifloxycoumarin or 3-bromo-4- tosyloxycoumarin provide an efficient and facile route for the synthesis of 3,4-disubstituted coumarins, which include 3,