dc.contributor.author | Mutai, Peggoty | |
dc.contributor.author | Breuzard, Gilles | |
dc.contributor.author | Pagano, Alessandra | |
dc.contributor.author | Allegro, Diane | |
dc.contributor.author | Peyrot, Vincent | |
dc.contributor.author | Chibale, Kelly | |
dc.date.accessioned | 2017-04-03T08:21:13Z | |
dc.date.available | 2017-04-03T08:21:13Z | |
dc.date.issued | 2017 | |
dc.identifier.citation | Bioorganic & Medicinal Chemistry Volume 25, Issue 5, 1 March 2017, Pages 1652–1665 | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/pii/S0968089616310732 | |
dc.identifier.uri | http://hdl.handle.net/11295/100751 | |
dc.description.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. | en_US |
dc.language.iso | en | en_US |
dc.publisher | University of Nairobi | en_US |
dc.title | Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents | en_US |
dc.type | Article | en_US |