Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid |
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| Authors: | Elke Persch Teodora Basile Svenja Bockelmann Markus Huss Helmut Wieczorek Teresa Carlomagno Dirk Menche |
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| Affiliation: | 1. Institut für Organische Chemie, Ruprecht-Karls-Universität Heidelberg, INF 270, 69120 Heidelberg, Germany;2. EMBL Heidelberg, Meyerhofstraße 1, 69117 Heidelberg, Germany;3. Universität Osnabrück, Fachbereich Biologie/Chemie, Abteilung Tierphysiologie, 49069 Osnabrück, Germany;4. Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121 Bonn, Germany |
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| Abstract: | The water-solubility of the highly potent V-ATPase inhibitors archazolid A and the glucosylated derivative archazolid C was studied in the presence of a wide range of cosolvents, revealing very low solubilites. The first water-soluble analogue was then designed, synthesized, and evaluated for V-ATPase inhibitory activity in vitro. |
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