Synthesis of novel dansyl-labeled Celecoxib derivatives |
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| Authors: | Andreas Lill Klaus Scholich Holger Stark |
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| Affiliation: | 1. Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany;2. Johann Wolfgang Goethe University, Institute of Clinical Pharmacology, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany;3. Heinrich-Heine-Universität Düsseldorf, Institute of Pharmaceutical and Medicinal Chemistry, Universitätsstraße 1, 40225 Düsseldorf, Germany |
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| Abstract: | Four novel dansyl-labeled derivatives of Celecoxib, a cyclooxygenase-2 (COX-2) selective inhibitor, were designed and synthesized. To realize the fluorophore-linker-approach divergent and convergent synthetic strategies were applied. Therefore Celecoxib p-benzoic acid, 8, was synthesized in a new and convenient way. The yield and the synthetic route to Celecoxib, 1, its pyrazolylic acid, 7, and its pyrazolylic methyl ester, 6, were improved. Through a convenient synthesis 1,11-diamino-3,6,9-trioxundecane, 19, was obtained in high yield and purity and used as a linker for the dansyl moiety. |
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| Keywords: | Fluorescence labeling Celecoxib Dansyl COX NSAR Linker |
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