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Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents

Peggoty Mutai Gilles Breuzard 1 Alessandra Pagano 1 Diane Allegro 1 Vincent Peyrot 1 Kelly Chibale 2
1 CRO2 - Centre de Recherches en Oncologie biologique et Oncopharmacologie
2 Department of Chemistry
Abstract : The synthesis of twenty-six 4-arylcoumarin analogues of combretastatin A-4 (CA-4) led to the identification of two new compounds (25 and 26) with strong cytotoxic activity. Both compounds had a high cytotoxic effect on a CA-4-resistant colon adenocarcinoma cell line (HT29D4). The compounds affected cell cycle progression characterized by a mitotic block. The activity of these compounds against microtubules both in vitro and in cells was examined and both compounds were found to potently inhibit in vitro microtubule formation via a sub-stoichiometric mode like CA-4. By immunofluorescence, it was observed that both compounds induced strong microtubule network disruption. Our results provide a strong experimental basis to develop new potent anti-tubulin molecules targeting CA-4-resistant cancer cells.
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https://hal-amu.archives-ouvertes.fr/hal-01744155
Contributor : Ludovic Leloup <>
Submitted on : Tuesday, March 27, 2018 - 10:46:16 AM
Last modification on : Thursday, June 20, 2019 - 9:52:06 AM

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Peggoty Mutai, Gilles Breuzard, Alessandra Pagano, Diane Allegro, Vincent Peyrot, et al.. Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents. Bioorganic and Medicinal Chemistry, Elsevier, 2017, 25 (5), pp.1652 - 1665. ⟨10.1016/j.bmc.2017.01.035⟩. ⟨hal-01744155⟩

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