Synthesis of anti-microtubule biaryls and preliminary evaluation as vascular-disrupting agents. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue ChemMedChem Année : 2008

Synthesis of anti-microtubule biaryls and preliminary evaluation as vascular-disrupting agents.

Résumé

A series of new dibenzoxepines were synthesized in a straightforward and efficient manner through diastereoselective biaryl Suzuki-Miyaura coupling and Br?ed-acid-mediated cyclodehydration as key steps. The vascular-disrupting potential of these molecules was evaluated with various in vitro assays: inhibition of microtubule assembly, antiproliferative activity against cancer cell lines and normal endothelial cells, modification of endothelial cell morphology, and disruption of endothelial cell cords. Two of these compounds showed promising activities in these assays, with profiles similar to that of the reference drug NAC and markedly different from that of colchicine. Altogether, these results show that dibenzoxepines represent promising new leads for the development of more selective vascular-disrupting agents.
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Dates et versions

hal-00342035 , version 1 (26-11-2008)

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Agnès Joncour, Jian-Miao Liu, Anne Décor, Sylviane Thoret, Joanna Wdzieczak-Bakala, et al.. Synthesis of anti-microtubule biaryls and preliminary evaluation as vascular-disrupting agents.. ChemMedChem, 2008, 3 (11), pp.1731-9. ⟨10.1002/cmdc.200800181⟩. ⟨hal-00342035⟩
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