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

Autor(en): Menche, Dirk 
Hassfeld, Jorma
Sasse, Florenz
Huss, Markus 
Wieczorek, Helmut 
Stichwörter: analogues; ARCHANGIUM-GEPHYRA; archazolid; Chemistry; Chemistry, Medicinal; Chemistry, Organic; H+-ATPASE; MEMBRANE; modeling; MOLECULAR MECHANICS; Pharmacology & Pharmacy; structure-activity data; SUBUNIT; V-ATPase; VACUOLAR-TYPE ATPASE
Erscheinungsdatum: 2007
Herausgeber: PERGAMON-ELSEVIER SCIENCE LTD
Journal: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volumen: 17
Ausgabe: 6
Startseite: 1732
Seitenende: 1735
Zusammenfassung: 
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. (c) 2006 Elsevier Ltd. All rights reserved.
ISSN: 0960894X
DOI: 10.1016/j.bmcl.2006.12.073

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