68217-95-8Relevant academic research and scientific papers
Discovery and optimization of novel 3-piperazinylcoumarin antagonist Of chemokine-like factor 1 with oral antiasthma activity in mice
Li, Gang,Wang, Dongmei,Sun, Mingna,Li, Guangyan,Hu, Jinfeng,Zhang, Yun,Yuan, Yuhe,Ji, Haijie,Chen, Naihong,Liu, Gang
experimental part, p. 1741 - 1754 (2010/08/06)
Chemokine-like factor 1 (CKLF1) is a novel functional cytokine that acts through its receptor CC chemokine receptor 4 (CCR4). Activation of CCR4 by CKLF1 plays an important role in diseases such as asthma and multiple sclerosis. This article describes a cell-based screening assay using an FITC-labeled CCR4 agonist (CKLF1-C27), a CKLF1 peptide fragment. Screening of our in-stock smallmolecule library identified a 3-piperazinylcoumarin analogue 1 (IC 50 = 4.36 × 10-6 M) that led to the discovery of orally active compound, 41 (IC50 = 2.12 × 10-8 M) through systematic optimization. Compound 41 blocked the calcium mobilization and Chemotaxis induced, by CKLF1-C27 and reduced the asthmatic pathologic changes in lung tissue of human CKLF1-transfected mice. Further studies indicated that compound 41 ameliorated pathological changes via inhibition of the NF-κB signal pathway.
A New and Convenient Synthesis of 4-Methyl-3-phenylcoumarins and 3-Phenylcoumarins
Neelakantan, S.,Raman, P. V.,Tinabaye, A.
, p. 256 - 257 (2007/10/02)
The reaction between ortho-hydroxyacetophenones and phenylacetyl chloride in acetone medium under the influence of potassium carbonate gives 4-methyl-3-phenylcoumarins exclusively.Under identical conditions, aromatic ortho-hydroxyaldehydes yield 3-phenylcoumarins smoothly.The reaction of aromatic ortho-hydroxy-carboxylic acid esters has also been examined.
