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.
9-Fluorenone-2-carboxylic acid as scaffold for tubulin interacting compounds / F. Calogero, S. Borrelli, G. Speciale, M.S. Christodoulou, D. Cartelli, D. Ballinari, F. Sola, C. Albanese, A. Ciavolella, D. Passarella, G. Cappelletti, S. Pieraccini, M. Sironi. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 78:7(2013), pp. 663-669. [Epub ahead of print] [10.1002/cplu.201300036]
9-Fluorenone-2-carboxylic acid as scaffold for tubulin interacting compounds
F. Calogero;S. Borrelli;M.S. Christodoulou;D. Cartelli;D. Passarella;G. Cappelletti;S. Pieraccini;M. Sironi
2013
Abstract
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.
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