208261-87-4Relevant academic research and scientific papers
Compositions containing five-membered unsaturated heterocyclic structure of the α, β unsaturated ketone compound and its preparation method and application
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Paragraph 0308, (2017/07/14)
The invention provides alpha, beta unsaturated ketone compounds containing benzo five-membered unsaturated heterocycle structures as well as a preparation method and an application and use of the compounds. The alpha, beta unsaturated ketone compounds containing the benzo five-membered unsaturated heterocycle structures have the structure of a formula (I). In addition, the invention further provides a method for preparing the compounds and a pharmaceutical composition containing the components as active components. In vitro activity tests show that the compounds provided by the invention show a remarkable inhibiting effect on tumor cells. Therefore, the invention lays a foundation for lucubrating and developing anti-tumor medicines in the future and meanwhile further provides a new technical means for treating tumor diseases.
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3
Hayes, Martin E.,Wallace, Grier A.,Grongsaard, Pintipa,Bischoff, Agnieszka,George, Dawn M.,Miao, Wenyan,McPherson, Michael J.,Stoffel, Robert H.,Green, David W.,Roth, Gregory P.
, p. 1573 - 1576 (2008/09/21)
High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.
Bicyclic aryl carboxamides and their therapeutic use
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Page column 11, (2010/02/05)
Compounds of the formula (i) have therapeutic utility via inhibition of TNF or phosphodiesterase.
