9-Fluorenone-2-Carboxylic Acid as a Scaffold for Tubulin Interacting Compounds

The introduction of a hydrophobic group at position 7 of 9‐fluorenone‐2‐carboxylic acid generates new tubulin binders, the design of which is suggested by modeling studies. The synthesis is based on the use of 2,7‐dibromo‐fluorenone as starting material. The antiproliferative activity on two differe...

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Bibliographic Details
Published in:ChemPlusChem (Weinheim, Germany) Germany), 2013-07, Vol.78 (7), p.663-669
Main Authors: Calogero, Francesco, Borrelli, Stella, Speciale, Gaetano, Christodoulou, Michael S., Cartelli, Daniele, Ballinari, Dario, Sola, Francesco, Albanese, Clara, Ciavolella, Antonella, Passarella, Daniele, Cappelletti, Graziella, Pieraccini, Stefano, Sironi, Maurizio
Format: Article
Language:English
Subjects:
2,7‐disubstituted fluorenones
7-disubstituted fluorenones
9-fluorenone-2-carboxylic acid
antitumor agents
docking
tubulins
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Summary:The introduction of a hydrophobic group at position 7 of 9‐fluorenone‐2‐carboxylic acid generates new tubulin binders, the design of which is suggested by modeling studies. The synthesis is based on the use of 2,7‐dibromo‐fluorenone as starting material. The antiproliferative activity on two different cell lines, fluorescent microscopy, flow cytometry, and sedimentation assay tests confirmed the supposed mechanism. Tubulin as the target: The introduction of a hydrophobic group at position 7 of 9‐fluorenone‐2‐carboxylic acid (see structure) generates new tubulin binders, the design of which is suggested by modeling studies. The antiproliferative activity on two different cell lines, fluorescent microscopy, flow cytometry, and sedimentation assay tests confirmed the supposed mechanism.
ISSN:2192-6506
2192-6506
DOI:10.1002/cplu.201300036