2. Academic Validation
  3. Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents

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

  • Bioorg Med Chem. 2017 Mar 1;25(5):1652-1665. doi: 10.1016/j.bmc.2017.01.035.
Peggoty Mutai 1,  Gilles Breuzard 2,  Alessandra Pagano 2,  Diane Allegro 2,  Vincent Peyrot 3,  Kelly Chibale 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Department of Pharmacology & Pharmacognosy, College of Health Sciences, University of Nairobi, PO Box 19676-00202, Nairobi, Kenya.
  • 2 Aix-Marseille Université, INSERM UMR_S 911 CRO2, Faculté de Pharmacie, 27 bd Jean-Moulin, 13385 Marseille, France.
  • 3 Aix-Marseille Université, INSERM UMR_S 911 CRO2, Faculté de Pharmacie, 27 bd Jean-Moulin, 13385 Marseille, France. Electronic address: vincent.peyrot@univ-amu.fr.
  • 4 Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address: Kelly.Chibale@uct.ac.za.
PMID: 28174064 DOI: 10.1016/j.bmc.2017.01.035
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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