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Bioorg Med Chem Lett. 2007 Mar 15;17(6):1732-5. Epub 2006 Dec 24.

Design, synthesis, and biological evaluation of novel analogues of archazolid: a highly potent simplified V-ATPase inhibitor.

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  • 1Helmholtz-Zentrum für Infektionsforschung GmbH, Medizinische Chemie, Inhoffenstrasse 7, 38124 Braunschweig, Germany. dirk.menche@heimholtz-hzi.de


Novel analogues of the V-ATPase inhibitors archazolid A and B with modifications of the free hydroxyl groups and the side chain were designed by molecular modeling, synthesized by derivatization of the parent natural product and evaluated for V-ATPase inhibition and growth inhibition of murine connective tissue cells.

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