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À propos de : Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones asFlavopiridol Mimics        

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  • Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones asFlavopiridol Mimics
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  • Novel 2-benzylidene-benzofuran-3-ones were designed and synthesized to mimic flavopiridol,a well-established inhibitor of cyclin-dependent kinases (CDKs) which is currently undergoingclinical evaluation. The underlying design concepts as well as the synthesis and structure−activity relationships (CDKs 1, 2, and 4 enzyme assays) of these mimics are described. Inhibitorsof CDKs 1 and 2 that are more potent and selective than flavopiridol were obtained.
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