71978-75-1

Upstream product

• 24672-82-0 1-[2,4-dihydroxy-3,5-bis-(3-methyl-but-2-enyl)-phenyl]-ethanone 
• 123-08-0 4-hydroxy-benzaldehyde 
• 89-84-9 2',4'-dihydroxy-4-acetophenone 
• 115-18-4 2-methyl-3-buten-2-ol 
• 1544322-35-1 1-(5-iodo-2,4-bis(methoxymethoxy)phenyl)ethanone 
• 6515-05-5 2',4'-bis(methoxymethoxy)acetophenone 

Relevant academic research and scientific papers

3,5-b isopentene base, 2, 4, 4 '-three hydroxy chalcone and its derivatives use and preparation

The invention discloses 3,5-diisoamylene, 2,4,4'-trihydroxyl chalcone as well as use and a preparation method of derivatives of the 3,5-diisoamylene, 2,4,4'-trihydroxyl chalcone, belonging to the field of a preparation method and anti-tumor activity measu

Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents

Licochalcone A (I), isolated from the roots of Chinese licorice, is the most promising antimalarial compound reported so far. In continuation of our drug discovery program, we isolated two similar chalcones, medicagenin (II) and munchiwarin (III), from Crotalaria medicagenia, which exhibited antimalarial activity against Plasmodium falciparum. A library of 88 chalcones were synthesized and evaluated for their in vitro antimalarial activity. Among these, 67, 68, 74, 77, and 78 exhibited good in vitro antimalarial activity against P. falciparum strains 3D7 and K1 with low cytotoxicity. These chalcones also showed reduction in parasitemia and increased survival time of Swiss mice infected with Plasmodium yoelii (strain N-67). Pharmacokinetic studies indicated that low oral bioavailability due to poor ADME properties. Molecular docking studies revealed the binding orientation of these inhibitors in active sites of falcipain-2 (FP-2) enzyme. Compounds 67, 68, and 78 showed modest inhibitory activity against the major hemoglobin degrading cysteine protease FP-2.