401504-46-9

Upstream product

• 621-23-8 1,2,3-trimethoxybenzene 
• 4672-74-6 propiolic acid anhydride 
• 59434-20-7 1,3,5-tri-O-benzylphloroglucinol 
• 637-44-5 phenylpropyolic acid 
• 407-25-0 trifluoroacetic anhydride 
• 471-25-0 Propiolic acid 
• 830-79-5 2,4,6-trimethoxybenzaldehyde 
• 832-58-6 1-(2,4,6-trimethoxyphenyl)ethanone 

Relevant academic research and scientific papers

Novel Chalcone Derivatives With Antimitotic Activity

The present invention relates to novel chalcone derivatives of formula (I): wherein X, Y, Z, W, RI, R2, R3, R4 and R5 are as defined, said derivatives having antimitotic activity, as well as to pharmaceutical compositions containing such compounds and to their use for making drugs.

Antimitotic and antiproliferative activities of chalcones: Forward structure-activity relationship

A series of 59 chalcones was prepared and evaluated for the antimitotic effect against K562 leukemia cells. The most active chalcones were evaluated for their antiproliferative activity against a panel of 11 human and murine cell cancer lines. We found that three chalcones were of great interest as potential antimitotic drugs. In vivo safety studies conducted on one of the most active chalcones revealed that the compound was safe, allowing further in vivo antitumor evaluation.

Synthesis, and cyclization to aurones and flavones, of alkoxy-substituted aryl, arylalkynyl ketones

Acylation of 1,3,5-tribenzyloxybenzene with alkoxy-substituted phenylpropioloyl chlorides provides the corresponding aryl alkoxylarylalkynyl ketones in which one of the benzyl groups has been removed. Cyclization of these phenolic ketones using basic reagents (potassium carbonate in acetone is best) provides the corresponding aurone system. When the phenolic group of the alkynyl ketones is protected as the t-butyldimethylsilyl ether followed by cyclization, using 18-crown-6 and potassium fluoride, mixtures of the corresponding aurones and flavones are produced. A by-product from the formation of the ketones is the corresponding β-chlorochalcone, which can also be cyclized to an aurone product using basic conditions. Similarly, the t-butyldimethylsilyl ethers of the HCl adducts can also be cyclized to a mixture of the corresponding aurones and flavones. CSIRO 2008.